Works (98)
Updated: August 12th, 2023 21:14
2022 journal article
2-Aminoimidazoles Inhibit Mycobacterium abscessus Biofilms in a Zinc-Dependent Manner
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 23(6).
author keywords: Mycobacterium abscessus; nontuberculous mycobacteria; biofilm; 2-aminoimidazoles; zinc
MeSH headings : Anti-Bacterial Agents / pharmacology; Biofilms; Humans; Imidazoles / pharmacology; Microbial Sensitivity Tests; Mycobacterium Infections, Nontuberculous; Mycobacterium abscessus; Zinc / pharmacology
TL;DR:
Preliminary mechanistic studies indicate that AB-2-29 acts through a distinct mechanism from those reported to date for 2-aminoimidazole compounds, and its antibiofilm activity is potentiated by the addition of zinc to the culture medium.
(via Semantic Scholar)
www.mdpi.com (publisher PDF)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: April 18, 2022
2021 journal article
Cheminformatics Analysis of Fluoroquinolones and Their Inhibition Potency Against Four Pathogens
MOLECULAR INFORMATICS, 40(5).
MeSH headings : Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Bacteria / drug effects; Cheminformatics; Drug Discovery; Escherichia coli / drug effects; Fluoroquinolones / chemistry; Fluoroquinolones / pharmacology; Microbial Sensitivity Tests; Pseudomonas aeruginosa / drug effects; Quantitative Structure-Activity Relationship; Staphylococcus aureus / drug effects; Streptococcus pneumoniae / drug effects
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: December 21, 2020
2019 journal article
2-aminoimidazoles collapse mycobacterial proton motive force and block the electron transport chain
SCIENTIFIC REPORTS, 9.
MeSH headings : Adenosine Triphosphate / metabolism; Antitubercular Agents / pharmacology; Biofilms / drug effects; Biofilms / growth & development; Electron Transport / drug effects; Humans; Imidazoles / pharmacology; Microbial Sensitivity Tests; Mycobacterium tuberculosis / drug effects; Mycobacterium tuberculosis / growth & development; Oxygen Consumption / drug effects; Proton-Motive Force / drug effects; Tuberculosis / drug therapy; Tuberculosis / microbiology
TL;DR:
The mechanism of action of 2-AIs against M. tuberculosis is elucidates, providing a tool to better understand mycob bacterial bioenergetics and develop compounds with improved anti-mycobacterial activity.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: February 25, 2019
2019 journal article
Identification of Anti-Mycobacterial Biofilm Agents Based on the 2-Aminoimidazole Scaffold
CHEMMEDCHEM, 14(9), 927–937.
author keywords: 2-aminoimidazoles; biofilms; mycobacteria; synergy; tuberculosis
MeSH headings : Animals; Antitubercular Agents / chemistry; Antitubercular Agents / pharmacology; Biofilms / drug effects; Imidazoles / chemistry; Male; Mice; Microsomes / drug effects; Microsomes / metabolism; Mycobacterium tuberculosis / drug effects
TL;DR:
Using Mycobacterium smegmatis as a surrogate organism, the identification of two new 2‐aminoimidazole compounds are reported that inhibit and disperse mycobacterial biofilms, work synergistically with isoniazid and rifampicin to eradicate preformed M.’smegmatisBiofilms in vitro, are nontoxic toward Galleria mellonella, and exhibit stability in mouse plasma.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: July 1, 2019
2019 journal article
Small Molecule Potentiation of Gram-Positive Selective Antibiotics against Acinetobacter baumannii
ACS INFECTIOUS DISEASES, 5(7), 1223–1230.
author keywords: antibiotic adjuvant; antibiotic resistance; Acinetobacter baumannii; macrolide antibiotics; glycopeptide antibiotics; lipopolysaccharide
MeSH headings : Acinetobacter Infections / drug therapy; Acinetobacter baumannii / drug effects; Animals; Anti-Bacterial Agents / administration & dosage; Anti-Bacterial Agents / pharmacology; Bacterial Outer Membrane / drug effects; Disease Models, Animal; Drug Resistance, Multiple, Bacterial / drug effects; Drug Synergism; Glycopeptides / administration & dosage; Glycopeptides / pharmacology; Macrolides / administration & dosage; Macrolides / pharmacology; Microbial Sensitivity Tests; Moths; Small Molecule Libraries / administration & dosage; Small Molecule Libraries / pharmacology
TL;DR:
Two adjuvant compounds are identified that dramatically enhance sensitivity of Acinetobacter baumannii to macrolide and glycopeptide antibiotics, with reductions in minimum inhibitory concentrations as high as 256-fold, and mode of action studies indicate that these adjuvants likely work by modulating lipopolysaccharide synthesis or assembly.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 5, 2019
2019 journal article
Using 2-aminobenzimidazole derivatives to inhibit Mycobacterium smegmatis biofilm formation
MEDCHEMCOMM, 10(3), 456–459.
TL;DR:
A series of 2-aminobenzimidazole (2-ABI) derivatives that potently inhibit biofilm formation by Mycobacterium smegmatis are reported on.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: April 22, 2019
2019 journal article
Using Small-Molecule Adjuvants to Repurpose Azithromycin for Use against Pseudomonas aeruginosa
ACS INFECTIOUS DISEASES, 5(1), 141–151.
author keywords: antibiotic resistance; antibiotic adjuvant; cystic fibrosis; Pseudomonas aeruginosa
MeSH headings : Adjuvants, Pharmaceutic / chemistry; Animals; Anti-Bacterial Agents / pharmacology; Azithromycin / pharmacology; Benzimidazoles / chemistry; Benzimidazoles / pharmacology; Cystic Fibrosis / drug therapy; Cystic Fibrosis / microbiology; Disease Models, Animal; Drug Repositioning; Larva / drug effects; Larva / microbiology; Microbial Sensitivity Tests; Moths / drug effects; Moths / microbiology; Pseudomonas aeruginosa / drug effects; Respiratory Tract Infections / drug therapy
TL;DR:
A novel approach to combatting pseudomonal infections through the use of bis-2-aminoimidazole adjuvants that can potentiate the activity of a macrolide antibiotic commonly prescribed to CF patients as an anti-inflammatory agent is described.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: April 20, 2020
2018 review
Narrow-spectrum antibacterial agents
[Review of ]. MEDCHEMCOMM, 9(1), 12–21.
TL;DR:
The advantages and challenges of narrow-Spectrum antibacterial agents are outlined, the progress that has been made toward developing diagnostics to enable their use is discussed, and some of the narrow-spectrum antib bacterial agents currently being investigated against some ofThe most clinically important bacteria including Clostridium difficile, Mycobacterium tuberculosis and several ESKAPE pathogens are described.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2018 journal article
Re-sensitizing Multidrug Resistant Bacteria to Antibiotics by Targeting Bacterial Response Regulators: Characterization and Comparison of Interactions between 2-Aminoimidazoles and the Response Regulators BfmR from Acinetobacter baumannii and QseB from Francisella spp.
FRONTIERS IN MOLECULAR BIOSCIENCES, 5.
author keywords: biofilms; antibiotic resistance; two-component systems; response regulators; Acinetobacter baumannii; Francisella
TL;DR:
This work investigates the response regulator/2-AI interaction and looks at a wider library of 2-AI compounds, and establishes that Francisella tularensis/novicida, encoding for only three known response regulators, can be a model system to study the interaction between 2-AIs and response regulators.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: January 28, 2019
2017 journal article
2-aminoimidazoles potentiate beta-lactam antimicrobial activity against Mycobacterium tuberculosis by reducing beta-lactamase secretion and increasing cell envelope permeability
PLoS One, 12(7).
Source: NC State University Libraries
Added: August 6, 2018
2017 journal article
Electrolyte-sensing transistor decals enabled by ultrathin microbial nanocellulose
Scientific Reports, 7.
Source: NC State University Libraries
Added: August 6, 2018
2017 journal article
Evaluation of a 2-aminoimidazole variant as adjuvant treatment for dermal bacterial infections
Drug Design Development and Therapy, 11, 153–162.
Source: NC State University Libraries
Added: August 6, 2018
2017 journal article
Probing the Mechanism of LAL-32, a Gold Nanoparticle-Based Antibiotic Discovered through Small Molecule Variable Ligand Display
BIOCONJUGATE CHEMISTRY, 28(7), 1807–1810.
MeSH headings : Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Cell Division / drug effects; Drug Discovery / methods; Drug Resistance, Bacterial; Escherichia coli / cytology; Escherichia coli / drug effects; Escherichia coli Proteins / antagonists & inhibitors; Gold; Ligands; Membrane Transport Proteins; Metal Nanoparticles / chemistry; Metal Nanoparticles / therapeutic use; Small Molecule Libraries
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2017 journal article
Small molecule adjuvants that suppress both chromosomal and mcr-1 encoded colistin-resistance and amplify colistin efficacy in polymyxin-susceptible bacteria
BIOORGANIC & MEDICINAL CHEMISTRY, 25(20), 5749–5753.
MeSH headings : Acinetobacter baumannii / drug effects; Adjuvants, Pharmaceutic / chemistry; Adjuvants, Pharmaceutic / pharmacology; Colistin / pharmacology; Drug Resistance, Bacterial / drug effects; Drug Resistance, Bacterial / genetics; Escherichia coli / drug effects; Escherichia coli Proteins / genetics; Escherichia coli Proteins / metabolism; Gram-Negative Bacteria / drug effects; Klebsiella pneumoniae / drug effects; Microbial Sensitivity Tests; Polymyxins / pharmacology; Small Molecule Libraries / chemistry; Small Molecule Libraries / pharmacology
TL;DR:
This work reports successful reversion of mcr-1-driven colistin resistance in Acinetobacter baumannii, Klebsiella pneumoniae, and Escherichia coli with adjuvants reported as modulators of chromosomally-encoded colistIn resistance.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2017 journal article
Structure of the Francisella response regulator QseB receiver domain, and characterization of QseB inhibition by antibiofilm 2-aminoimidazole-based compounds
MOLECULAR MICROBIOLOGY, 106(2), 223–235.
MeSH headings : Anti-Bacterial Agents / pharmacology; Bacterial Proteins / chemistry; Bacterial Proteins / metabolism; Bacterial Proteins / ultrastructure; Biofilms / drug effects; Francisella tularensis / metabolism; Gene Expression Regulation, Bacterial / genetics; Imidazoles / metabolism; Imidazoles / pharmacology; Protein Binding; Virulence / drug effects; Virulence Factors / genetics; Virulence Factors / metabolism
TL;DR:
It is shown that QseB interacts with 2‐aminoimidazole based compounds that impede its function, and this information will assist in tailoring compounds to act as adjuvants that will enhance the effect of antibiotics.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2017 journal article
Targeting of Streptococcus mutans Biofilms by a Novel Small Molecule Prevents Dental Caries and Preserves the Oral Microbiome
JOURNAL OF DENTAL RESEARCH, 96(7), 807–814.
author keywords: microbiota; rats; dental enamel; microscopy; bacteria; microbial ecology
MeSH headings : Animals; Biofilms / drug effects; Dental Caries / prevention & control; Dental Enamel / drug effects; Imidazoles / pharmacology; Microbiota / drug effects; Microscopy, Confocal; Polymerase Chain Reaction; Rats; Streptococcus gordonii / drug effects; Streptococcus mutans / drug effects; Streptococcus sanguis / drug effects
TL;DR:
It is demonstrated that selective targeting of S. mutans biofilms by 3F1 was able to effectively reduce dental caries in vivo without affecting the overall oral microbiota shaped by the intake of dietary sugars, suggesting that the pathogenic biofilm-specific treatment is a viable strategy for disease prevention.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2017 article
The Challenge of Overcoming Antibiotic Resistance: An Adjuvant Approach?
Melander, R. J., & Melander, C. (2017, August). ACS INFECTIOUS DISEASES, Vol. 3, pp. 559–563.
MeSH headings : Adjuvants, Pharmaceutic / pharmacology; Animals; Anti-Bacterial Agents / pharmacology; Drug Interactions; Drug Resistance, Bacterial / drug effects; Drug Resistance, Bacterial / physiology; Gram-Negative Bacteria / drug effects; Gram-Negative Bacteria / growth & development; Gram-Negative Bacteria / metabolism; Gram-Positive Bacteria / drug effects; Gram-Positive Bacteria / growth & development; Gram-Positive Bacteria / metabolism; Humans
TL;DR:
Some of the advantages and disadvantages of the use of adjuvants, and various approaches to their identification are described, which have the potential to render an antibiotic against which bacteria have developed resistance once again effective.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2017 journal article
The Discovery of 2-Aminobenzimidazoles That Sensitize Mycobacterium smegmatis and M. tuberculosis to beta-Lactam Antibiotics in a Pattern Distinct from beta-Lactamase Inhibitors
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 56(14), 3940–3944.
author keywords: aminobenzimidazoles; antibiotic resistance; medicinal chemistry; tuberculosis
MeSH headings : Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Benzimidazoles / chemistry; Benzimidazoles / pharmacology; Drug Discovery; Lactams / chemical synthesis; Lactams / chemistry; Lactams / pharmacology; Molecular Structure; Mycobacterium smegmatis / drug effects; Mycobacterium smegmatis / enzymology; Mycobacterium tuberculosis / drug effects; Mycobacterium tuberculosis / enzymology; beta-Lactamase Inhibitors / chemical synthesis; beta-Lactamase Inhibitors / chemistry; beta-Lactamase Inhibitors / pharmacology; beta-Lactamases / metabolism
TL;DR:
A library of 2-aminobenzimidazole derivatives was screened for the ability to suppress β-lactam resistance in Mycobacterium smegmatis and preliminary mechanistic studies revealed that the lead compounds act through a mechanism distinct from that of traditional β- lactamase inhibitors.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2016 journal article
Evaluation of ethyl N-(2-phenethyl) carbamate analogues as biofilm inhibitors of methicillin resistant Staphylococcus aureus
ORGANIC & BIOMOLECULAR CHEMISTRY, 14(28), 6853–6856.
MeSH headings : Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Biofilms / drug effects; Carbamates / chemistry; Carbamates / pharmacology; Humans; Methicillin-Resistant Staphylococcus aureus / drug effects; Methicillin-Resistant Staphylococcus aureus / physiology; Microbial Sensitivity Tests; Small Molecule Libraries / chemistry; Small Molecule Libraries / pharmacology; Staphylococcal Infections / drug therapy
TL;DR:
A small molecule library consisting of 45 compounds was synthesized based on the bacterial metabolite ethyl N-(2-phenethyl) carbamate which revealed a potent analogue capabale of inhibiting several strains of Methicillin Resistant S. aureus biofilms with low to moderate micromolar IC50 values.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2016 journal article
Marine sponge alkaloids as a source of anti-bacterial adjuvants
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 26(24), 5863–5866.
author keywords: Marine sponge; Pyrrole-imidazole alkaloid; Biofilm; Antibiotic; Adjuvant
MeSH headings : Acinetobacter baumannii / drug effects; Alkaloids / chemistry; Alkaloids / metabolism; Alkaloids / pharmacology; Animals; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / metabolism; Anti-Bacterial Agents / pharmacology; Dose-Response Relationship, Drug; Imidazoles / chemistry; Imidazoles / pharmacology; Methicillin-Resistant Staphylococcus aureus / drug effects; Microbial Sensitivity Tests; Molecular Structure; Porifera; Pyrroles / chemistry; Pyrroles / pharmacology; Structure-Activity Relationship
TL;DR:
The potential of marine secondary metabolites to serve as a source of non-traditional anti-bacterial agents is demonstrated by showing that pyrrole-imidazole alkaloids inhibit biofilm formation and suppress antibiotic resistance.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
14. Life Below Water
(OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2016 journal article
Potentiation of Francisella resistance to conventional antibiotics through small molecule adjuvants
MEDCHEMCOMM, 7(1), 128–131.
TL;DR:
A screen of 20 compounds identified small molecule adjuvants capable of potentiating anitbiotic activty against Francisella philomiragia and led to the discovery of a potentially new class of small molecule aduvants containg an indole core.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2016 journal article
Potentiation of the fosmidomycin analogue FR 900098 with substituted 2-oxazolines against Francisella novicida
MEDCHEMCOMM, 7(10), 1952–1956.
TL;DR:
A highly potent 2-oxazoline adjuvant was discovered capable of potentiating FR 900098 with a 1000-fold reduction in MIC against the Francisella sub-species F. novicida and F. philomiragia.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2016 journal article
Second generation modifiers of colistin resistance show enhanced activity and lower inherent toxicity
TETRAHEDRON, 72(25), 3549–3553.
author keywords: Antibiotic adjuvant; 2-Aminoimidazole; Colistin; ESKAPE pathogens; Acinetobacter baumannii; Pseudomonas aeruginosa
TL;DR:
From these libraries, a new small molecule was identified that lowers the minimum inhibitory concentration of colistin by up to 32-fold greater than the parent compound while also displaying less inherent bacterial effect, thereby minimizing the likelihood of resistance evolution.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2015 journal article
A new small molecule inhibits Streptococcus mutans biofilms invitro and in vivo
Journal of Applied Microbiology, 119(5), 1403–1411.
MeSH headings : Animals; Anti-Bacterial Agents / administration & dosage; Biofilms / drug effects; Dental Caries / microbiology; Female; Humans; Imidazoles / administration & dosage; Mice; Rats; Rats, Sprague-Dawley; Streptococcal Infections / drug therapy; Streptococcal Infections / microbiology; Streptococcus mutans / drug effects; Streptococcus mutans / physiology; Triazoles / administration & dosage
TL;DR:
The aim of this study was to identify new small molecules that can inhibit Streptococcus mutans biofilms by in vitro and in vivo model.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
14. Life Below Water
(OpenAlex)
Source: NC State University Libraries
Added: August 6, 2018
2015 journal article
Augmenting anti-cancer natural products with a small molecule adjuvant
Marine Drugs, 13(1), 65–75.
Source: NC State University Libraries
Added: August 6, 2018
2015 article
From Worms to Targeting Virulence Factors
Melander, R. J., & Melander, C. (2015, April 23). CHEMISTRY & BIOLOGY, Vol. 22, pp. 436–437.
MeSH headings : Animals; Bacterial Proteins / metabolism; Caenorhabditis elegans / microbiology; Metalloendopeptidases / metabolism; Pseudomonas aeruginosa / physiology; Virulence Factors / metabolism
TL;DR:
A Caenorhabditis elegans model is used to validate the Pseudomonas aeruginosa virulence factor LasB as a potential therapeutic target and to identify a LasB inhibitor with in-vivo efficacy.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2015 journal article
Gold nanoparticles to improve HIV drug delivery
FUTURE MEDICINAL CHEMISTRY, 7(9), 1097–1107.
MeSH headings : Animals; Anti-HIV Agents / administration & dosage; Anti-HIV Agents / chemical synthesis; Anti-HIV Agents / chemistry; Brain / metabolism; Drug Carriers / chemistry; Endothelial Cells / cytology; Endothelial Cells / drug effects; Endothelial Cells / metabolism; Female; Gold / chemistry; HIV Core Protein p24 / antagonists & inhibitors; HIV Core Protein p24 / metabolism; HIV Infections / drug therapy; HIV-1 / physiology; Humans; Leukocytes, Mononuclear / cytology; Leukocytes, Mononuclear / drug effects; Leukocytes, Mononuclear / metabolism; Macrophages / cytology; Macrophages / drug effects; Macrophages / metabolism; Metal Nanoparticles / chemistry; Metal Nanoparticles / toxicity; Metal Nanoparticles / ultrastructure; Mice; Mice, Inbred BALB C; Raltegravir Potassium / administration & dosage; Raltegravir Potassium / chemical synthesis; Raltegravir Potassium / chemistry; Tissue Distribution; Virus Replication / drug effects
TL;DR:
Gold nanoparticles prove to be a promising tool to use in HIV therapy by showing entry into different cell types, antiviral activity of an HIV integrase inhibitor conjugated in a gold nanoparticle and penetration into the brain in vivo without toxicity.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2015 journal article
Inhibition and breaking of advanced glycation end-products (AGEs) with bis-2-aminoimidazole derivatives
TETRAHEDRON LETTERS, 56(23), 3406–3409.
author keywords: Advanced glycation end-products (AGES); Bis-2-aminoimidazole; Aminoguanidine; Diabetes
TL;DR:
The screening of a series of 2-aminoimidazloles for anti-AGE activity is reported, and the identification of a bis-2-aminosidazole lead compound that possesses superior AGE inhibition and breaking activity compared to the known AGE inhibitor aminoguanidine is identified.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2015 journal article
Innovative strategies for combating biofilm-based infections
Biofilm-Based Healthcare-Associated Infections, Vol Ii, 831, 69–91.
Source: NC State University Libraries
Added: August 6, 2018
2015 journal article
Membrane-Permeabilizing Activity of Reverse-Amide 2-Aminoimidazole Antibiofilm Agents Against Acinetobacter baumannii
CURRENT DRUG DELIVERY, 12(2), 223–230.
author keywords: 2-aminoimidazole; Acinetobacter baumannii; biofilm; membrane permeabilization; reverse amide; SEM
MeSH headings : Acinetobacter baumannii / drug effects; Amides / chemistry; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Biofilms / drug effects; Cell Membrane Permeability / drug effects; Cells, Cultured; Cross Infection; Imidazoles / chemistry; Imidazoles / pharmacology; Microbial Sensitivity Tests
TL;DR:
A model is proposed that describes how the structure of RA-2AI allows it to insert itself into and disrupt the fluidity of the membrane, creating an opportunity for increased molecular permeability.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2015 journal article
Second generation 2-aminoimidazole based advanced glycation end product inhibitors and breakers
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 25(21), 4820–4823.
author keywords: Advanced glycation end-product (AGE); 2-Aminoimidazole; Akabori; Diabetes
MeSH headings : Glycation End Products, Advanced / antagonists & inhibitors; Glycation End Products, Advanced / metabolism; Imidazoles / chemical synthesis; Imidazoles / chemistry; Imidazoles / pharmacology; Molecular Structure; Structure-Activity Relationship
TL;DR:
The use of a rapid, scalable, two-step procedure is reported to access a second generation of 2-AI based anti-AGE compounds from commercially available amino acids that exhibit increased AGE inhibition and breaking activty compared to the first generation compounds.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2014 journal article
Controlling bacterial behavior with indole-containing natural products and derivatives
TETRAHEDRON, 70(37), 6363–6372.
author keywords: Indole; Bacterial communication; Anti-virulence; Biofilm; Antibiotic resistance
TL;DR:
An overview of the process controlled by indole signaling is given, current efforts to design indole-containing small molecules to intercept these pathways are summarized, and the synthetic efforts towards accessing indole derived bioactive small molecules are detailed.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2014 journal article
Expression of antimicrobial drug tolerance by attached communities of Mycobacterium tuberculosis
PATHOGENS AND DISEASE, 70(3), 359–369.
author keywords: Mycobacterium tuberculosis; drug resistant; drug tolerant; biofilm; microbial communities
MeSH headings : Antitubercular Agents / pharmacology; Biofilms / drug effects; Biofilms / growth & development; Culture Media; Deoxyribonuclease I / metabolism; Drug Resistance, Bacterial / genetics; Gene Expression Regulation, Bacterial / drug effects; Humans; Isoniazid / pharmacology; Microbial Sensitivity Tests; Mycobacterium tuberculosis / drug effects; Mycobacterium tuberculosis / physiology; Polysorbates / pharmacology; Rifampin / pharmacology
TL;DR:
It is demonstrated that in vitro expression of drug tolerance by M. tuberculosis is linked to the establishment of attached microbial communities and that dispersion of bacilli targeting the extracellular matrix including DNA restores drug susceptibility.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2014 journal article
Nanoscale Structure-Activity Relationships, Mode of Action, and Biocompatibility of Gold Nanoparticle Antibiotics
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 136(14), 5295–5300.
MeSH headings : Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Biocompatible Materials / chemical synthesis; Biocompatible Materials / chemistry; Biocompatible Materials / pharmacology; Dose-Response Relationship, Drug; Drug Resistance, Multiple, Bacterial / drug effects; Escherichia coli / drug effects; Gold / chemistry; Gold / pharmacology; Klebsiella pneumoniae / drug effects; Metal Nanoparticles / chemistry; Microbial Sensitivity Tests; Structure-Activity Relationship
TL;DR:
It is shown that gold nanoparticles are also active against MDR E. coli and MDR Klebsiella pneumoniae, and resistance to these nanoparticles develops significantly more slowly than to a commercial small-molecule drug.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2014 journal article
Reversal of Mycobacterium tuberculosis phenotypic drug resistance by 2-aminoimidazole- based small molecules
PATHOGENS AND DISEASE, 70(3), 370–378.
author keywords: tuberculosis; drug tolerant; biofilm; 2-aminoimidazole; drug resistant; isoniazid
MeSH headings : Antitubercular Agents / chemistry; Antitubercular Agents / pharmacology; Biofilms / drug effects; Biofilms / growth & development; Drug Resistance, Bacterial; Humans; Imidazoles / chemistry; Imidazoles / pharmacology; Microbial Sensitivity Tests; Mycobacterium smegmatis / drug effects; Mycobacterium smegmatis / physiology; Mycobacterium tuberculosis / drug effects; Mycobacterium tuberculosis / physiology; Phenotype
TL;DR:
2-aminoimidazole-based small molecules as an adjunct to antimicrobial treatment has the potential to be an effective antituberculosis treatment strategy designed specifically to eradicate drug-tolerant M. tuberculosis.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2014 journal article
Small Molecule Downregulation of PmrAB Reverses Lipid A Modification and Breaks Colistin Resistance
ACS CHEMICAL BIOLOGY, 9(1), 122–127.
MeSH headings : Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Bacterial Proteins / genetics; Colistin / chemistry; Colistin / pharmacology; Down-Regulation / drug effects; Drug Resistance, Multiple, Bacterial / drug effects; Gram-Negative Bacteria / drug effects; Gram-Negative Bacteria / genetics; Gram-Negative Bacteria / metabolism; Gram-Negative Bacterial Infections / drug therapy; Humans; Lipid A / metabolism; Small Molecule Libraries / chemistry; Small Molecule Libraries / pharmacology; Transcription Factors / genetics
TL;DR:
This report reports a small molecule adjuvant that suppresses colistin resistance in multidrug resistant Acinetobacter baumannii and Klebsiella pneumoniae by interfering with the expression of a two-component system.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2014 journal article
Small-Molecule Suppression of beta-Lactam Resistance in Multidrug-Resistant Gram-Negative Pathogens
JOURNAL OF MEDICINAL CHEMISTRY, 57(17), 7450–7458.
MeSH headings : Animals; Cell Line; Cell Survival / drug effects; Drug Resistance, Multiple, Bacterial / drug effects; Gram-Negative Bacteria / classification; Gram-Negative Bacteria / drug effects; Hemolysis / drug effects; Humans; Keratinocytes / cytology; Keratinocytes / drug effects; Microbial Sensitivity Tests; Sheep; Small Molecule Libraries / chemistry; Small Molecule Libraries / pharmacology; beta-Lactam Resistance / drug effects
TL;DR:
A small molecule was identified from this library of aryl amide 2-aminoimidazoles that is capable of lowering the minimum inhibitory concentration of β-lactam antibiotics by up to 64-fold.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2014 journal article
Thiol-modified gold nanoparticles for the inhibition of Mycobacterium smegmatis
CHEMICAL COMMUNICATIONS, 50(100), 15860–15863.
MeSH headings : Cell Line; Cell Survival / drug effects; Erythrocytes / cytology; Erythrocytes / drug effects; Gold / chemistry; Hemolysis / drug effects; Humans; Metal Nanoparticles / chemistry; Metal Nanoparticles / toxicity; Microbial Sensitivity Tests; Mycobacterium smegmatis / drug effects; Sulfhydryl Compounds / chemistry
TL;DR:
It is demonstrated that the Small Molecule Variable Ligand Display (SMLVD) method for nanoparticle antibiotic discovery can be expanded around a ligand feed ratio parameter space to identify gold nanoparticle conjugates that are potent inhibitors of mycobacteria growth.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2013 journal article
A flexible approach to 1,4-di-substituted 2-aminoimidazoles that inhibit and disperse biofilms and potentiate the effects of beta-lactams against multi-drug resistant bacteria
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 62, 59–70.
author keywords: Biofilms; MRSA; Suppression of antibiotic resistance; 2-Aminoimidazoles
MeSH headings : Biofilms / drug effects; Dose-Response Relationship, Drug; Imidazoles / chemical synthesis; Imidazoles / chemistry; Imidazoles / pharmacology; Methicillin-Resistant Staphylococcus aureus / drug effects; Molecular Structure; Structure-Activity Relationship; beta-Lactams / chemistry; beta-Lactams / pharmacology
TL;DR:
These 2-AITs were found to inhibit biofilm formation by MRSA with low micromolar IC50 values and acted synergistically with oxacillin against MRSA lowering the minimum inhibitory concentration (MIC) 4-fold.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2013 journal article
Biologically inspired strategies for combating bacterial biofilms
CURRENT OPINION IN PHARMACOLOGY, 13(5), 699–706.
MeSH headings : Animals; Anti-Bacterial Agents / pharmacology; Anti-Bacterial Agents / therapeutic use; Bacterial Infections / drug therapy; Bacterial Infections / metabolism; Bacterial Physiological Phenomena / drug effects; Biofilms / drug effects; Humans; Quorum Sensing / drug effects; Signal Transduction / drug effects
TL;DR:
Small molecule interference with bacterial communication and signaling pathways, including quorum sensing and two-component signal transduction systems are focused on, focusing firstly on enzymatic approaches to the degradation of extracellular matrix components to effect biofilm dispersal.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2013 review
Combination approaches to combat multidrug-resistant bacteria
[Review of ]. TRENDS IN BIOTECHNOLOGY, 31(3), 177–184.
author keywords: antibiotic resistance; antibiotic adjuvant
MeSH headings : Adjuvants, Pharmaceutic / therapeutic use; Anti-Bacterial Agents / therapeutic use; Bacterial Infections / drug therapy; Bacterial Infections / microbiology; Drug Resistance, Multiple, Bacterial; Drug Therapy, Combination / methods; Humans
TL;DR:
Recent developments toward combination therapies for the treatment of multidrug-resistant bacterial infections are described, and the development of adjuvants that either directly target resistance mechanisms such as the inhibition of β-lactamase enzymes, or indirectly target resistance by interfering with bacterial signaling pathways such as two-component systems (TCSs).
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2013 journal article
Highly Active Modulators of Indole Signaling Alter Pathogenic Behaviors in Gram-Negative and Gram-Positive Bacteria
CHEMISTRY-A EUROPEAN JOURNAL, 19(51), 17595–17602.
author keywords: desformylflustrabromine; mechanistic probes; natural products; phenotype control; structure-activity relationships
MeSH headings : Bacterial Proteins / antagonists & inhibitors; Bacterial Proteins / metabolism; Biofilms / drug effects; Gram-Negative Bacteria / drug effects; Gram-Negative Bacteria / physiology; Gram-Positive Bacteria / drug effects; Gram-Positive Bacteria / physiology; Hydrocarbons, Brominated / chemical synthesis; Hydrocarbons, Brominated / chemistry; Hydrocarbons, Brominated / pharmacology; Indole Alkaloids / chemical synthesis; Indole Alkaloids / chemistry; Indole Alkaloids / pharmacology; Indoles / chemical synthesis; Indoles / chemistry; Indoles / pharmacology; Phenotype; Structure-Activity Relationship; Temperature; Trans-Activators / antagonists & inhibitors; Trans-Activators / metabolism; Tryptophanase / antagonists & inhibitors; Tryptophanase / metabolism
TL;DR:
This investigation demonstrates that molecules based on the dFBr scaffold can alter pathogenic behaviors by mimicking indole-signaling pathways and develop non-microbicidal dF Br derivatives that are 27-2000 times more active than indole in modulating biofilm formation, motility, acid resistance, and antibiotic resistance.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2013 journal article
Indole-triazole conjugates are selective inhibitors and inducers of bacterial biofilms
MEDCHEMCOMM, 4(6), 916–919.
TL;DR:
Structural/function studies revealed that the addition of a bromine atom at the 2-position of the indole/triazole scaffold altered activity against both Gram-negative and Gram-positive bacteria and could transform a biofilm inhibitor into aBiofilm inducer.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2013 journal article
N-Substituted 2-aminoimidazole inhibitors of MRSA biofilm formation accessed through direct 1,3-bis(tert-butoxycarbonyl)guanidine cyclization
ORGANIC & BIOMOLECULAR CHEMISTRY, 11(1), 130–137.
MeSH headings : Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Biofilms / drug effects; Biofilms / growth & development; Cyclization; Guanidines / chemistry; Imidazoles / chemical synthesis; Imidazoles / chemistry; Imidazoles / pharmacology; Methicillin-Resistant Staphylococcus aureus / drug effects; Molecular Structure; Structure-Activity Relationship; Triazoles / chemical synthesis; Triazoles / chemistry; Triazoles / pharmacology
TL;DR:
A library of N-substituted derivatives of a previously reported 2-aminoimidazole/triazole (2-AIT) biofilm modulator exhibited synergistic activity with oxacillin against planktonic MRSA and has the potential to be used as adjuvants with conventional antibiotics.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2013 journal article
Overcoming Resistance to beta-Lactam Antibiotics
JOURNAL OF ORGANIC CHEMISTRY, 78(9), 4207–4213.
MeSH headings : Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Drug Discovery; Molecular Structure; Small Molecule Libraries / chemical synthesis; Small Molecule Libraries / chemistry; Small Molecule Libraries / pharmacology; beta-Lactam Resistance / drug effects; beta-Lactamase Inhibitors; beta-Lactams / chemical synthesis; beta-Lactams / chemistry; beta-Lactams / pharmacology
TL;DR:
Small molecule strategies to overcome resistance to β-lactam antibiotics include the development of β- lactamase inhibitors and compounds that interfere with the ability of the bacteria to sense an antibiotic threat and activate their resistance mechanisms.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2013 journal article
Programmable DNA-binding small molecules
BIOORGANIC & MEDICINAL CHEMISTRY, 21(20), 6101–6114.
author keywords: Polyamide; Transcription; Minor groove; DNA binding
MeSH headings : Animals; DNA / chemistry; DNA / drug effects; DNA / genetics; Gene Expression / drug effects; Humans; Imidazoles / chemistry; Imidazoles / pharmacology; Pyrroles / chemistry; Pyrroles / pharmacology
TL;DR:
A brief history of early seminal developments in the field is presented and recent reports of the utility of polyamides as both genetic modulators and molecular probes are highlighted.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2013 review
Small-molecule inhibition of bacterial two-component systems to combat antibiotic resistance and virulence
[Review of ]. FUTURE MEDICINAL CHEMISTRY, 5(11), 1265–1284.
MeSH headings : Bacteria / metabolism; Bacteria / pathogenicity; Bacterial Infections / drug therapy; Bacterial Proteins / antagonists & inhibitors; Bacterial Proteins / metabolism; Biofilms / drug effects; Drug Resistance, Multiple, Bacterial / drug effects; Histidine Kinase; Humans; Protein Kinases / chemistry; Protein Kinases / metabolism; Signal Transduction / drug effects; Small Molecule Libraries / chemistry; Small Molecule Libraries / pharmacology; Small Molecule Libraries / therapeutic use; Virulence / drug effects
TL;DR:
An overview of TCS that are potential targets for such a strategy, small-molecules inhibitors of T CS identified to date are described, and assays for the identification of novel inhibitors are discussed.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2012 journal article
2-Aminopyrimidine as a novel scaffold for biofilm modulation
Organic & Biomolecular Chemistry, 10(13), 2552–2561.
Source: NC State University Libraries
Added: August 6, 2018
2012 journal article
A modular approach to the synthesis of 1,4,5-substituted-2-aminoimidazoles
TETRAHEDRON LETTERS, 53(10), 1204–1206.
author keywords: N-H insertion; 2-Aminoimidazole; Antibiotic; Polysubstitution; Heterocycle
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2012 journal article
Deconvoluting Interspecies Bacterial Communication
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 51(26), 6314–6315.
author keywords: autoinducer-2; bacterial communication; 4; 5-dihydroxy-2; 3-pentanedione; NMR spectroscopy; quorum sensing
MeSH headings : Bacteria / chemistry; Pentanes / analysis; Quorum Sensing; Signal Transduction
TL;DR:
NMR spectroscopy has now been used to establish that the extent of the structural diversity displayed by DPD over a broad pH range is even greater than previously posited.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
15. Life on Land
(OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2012 journal article
Evaluation of the toxicity of 2-aminoimidazole antibiofilm agents using both cellular and model organism systems
DRUG AND CHEMICAL TOXICOLOGY, 35(3), 310–315.
author keywords: 2-aminoimidazole; adjuvant; biofilm; Caenorhabditis elegans; toxicity; Toxicity of 2-aminoimidazole; antibiofilm agents
MeSH headings : Adjuvants, Pharmaceutic / toxicity; Animals; Anti-Bacterial Agents / pharmacology; Anti-Bacterial Agents / toxicity; Biofilms / drug effects; Caenorhabditis elegans; Cell Line; Dose-Response Relationship, Drug; Environmental Exposure; Fertility / drug effects; Humans; Imidazoles / pharmacology; Imidazoles / toxicity; Keratinocytes / metabolism; Tetrazolium Salts; Thiazoles; Toxicity Tests
TL;DR:
The most effective antibiofilm compound had significant effects when used in conjunction with several standard antibiotics against resistant bacteria and was found to maintain the same low level of toxicity as when acting alone, bolstering its candidacy for further testing as an adjuvant.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2012 journal article
Foliar-Applied Small Molecule that Suppresses Biofilm Formation and Enhances Control of Copper-Resistant Xanthomonas euvesicatoria on Pepper
PLANT DISEASE, 96(11), 1638–1644.
TL;DR:
A small molecule additive, a member of the 2-aminoimidazole (2AI) group that is an analogue of the marine sponge natural product oroidin that suppresses resistance of Xanthomonas euvesicatoria to copper and decreases biofilm formation in an in vitro system is reported.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
14. Life Below Water
(OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2012 journal article
H-1, C-13, and N-15 resonance assignments and secondary structure prediction of the full-length transition state regulator AbrB from Bacillus anthracis
BIOMOLECULAR NMR ASSIGNMENTS, 6(1), 95–98.
author keywords: AbrB; NMR; Bacillus anthracis; Transition state regulator
MeSH headings : Bacillus anthracis; Bacterial Proteins / chemistry; DNA-Binding Proteins / chemistry; Nuclear Magnetic Resonance, Biomolecular; Protein Structure, Secondary; Transcription Factors / chemistry
TL;DR:
Backbone and sidechain resonance assignments and secondary structure prediction for the full-length AbrB protein from B. anthracis are reported.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2012 journal article
Identification of BfmR, a Response Regulator Involved in Biofilm Development, as a Target for a 2-Aminoimidazole-Based Antibiofilm Agent
BIOCHEMISTRY, 51(49), 9776–9778.
MeSH headings : Acinetobacter baumannii / drug effects; Acinetobacter baumannii / growth & development; Bacterial Proteins / chemistry; Bacterial Proteins / physiology; Biofilms / drug effects; Imidazoles / pharmacology; Microscopy, Confocal; Models, Molecular
TL;DR:
The 2AI compound studied here represents a unique small molecule scaffold that targets bacterial response regulators and is cell permeable, while pull-down assays identified BfmR, a response regulator that is the master controller of biofilm formation, as a target for this compound.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2012 journal article
Medicinal chemistry: Forcing an enemy into the open
Nature Chemistry, 4(9), 692–693.
Source: NC State University Libraries
Added: August 6, 2018
2012 journal article
Potent Small-Molecule Suppression of Oxacillin Resistance in Methicillin-Resistant Staphylococcus aureus
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 51(45), 11254–11257.
author keywords: 2-aminoimidazoles; adjuvants; antibiotics; antibiotic resistance; MRSA
MeSH headings : Anti-Bacterial Agents / pharmacology; Drug Resistance; Methicillin-Resistant Staphylococcus aureus / drug effects; Microbial Sensitivity Tests; Oxacillin / pharmacology
TL;DR:
A potent small molecule is pictured that, at sub-minimum inhibitory concentration levels, lowers the MIC of oxacillin against a number of MRSA strains by up to 512-fold.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2012 journal article
Small Molecule Suppression of Carbapenem Resistance in NDM-1 Producing Klebsiella pneumoniae
ACS MEDICINAL CHEMISTRY LETTERS, 3(5), 357–361.
author keywords: NDM-1; Klebsiella pneumoniae; antibiotic adjuvant; resistance suppression; 2-aminoimidazole
TL;DR:
A 2-aminoimidazole derived small molecule is identified that acts as an antibiotic adjuvant and is able to suppress resistance of a NDM-1 producing strain of K. pneumoniae, able to lower carbapenem minimum inhibitory concentrations by up to 16-fold while exhibiting little bactericidal activity itself.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2012 journal article
Small molecule control of bacterial biofilms
Organic & Biomolecular Chemistry, 10(37), 7457–7474.
Source: NC State University Libraries
Added: August 6, 2018
2012 journal article
Synthesis of Guanidinium Functionalized Polycarbodiimides and Their Antibacterial Activities
ACS MACRO LETTERS, 1(3), 370–374.
TL;DR:
These polycarbodiimide-guanidinium-triazole conjugates offered moderate to significant antibacterial activity and rapid interaction with red blood cells causing blood precipitation without significant hemolysis in case of Poly-2(b-e).
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
6. Clean Water and Sanitation
(OpenAlex)
Sources: Web Of Science, ORCID, NC State University Libraries
Added: August 6, 2018
2011 journal article
A New Small Molecule Specifically Inhibits the Cariogenic Bacterium Streptococcus mutans in Multispecies Biofilms
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 55(6), 2679–2687.
MeSH headings : Adhesins, Bacterial / analysis; Anti-Bacterial Agents / pharmacology; Biofilms / drug effects; Gene Expression Profiling; Streptococcus mutans / drug effects; Streptococcus mutans / genetics; Streptococcus mutans / growth & development
TL;DR:
In multispecies biofilm models, the most active compound also inhibited cell survival and biofilm formation of S. mutans but did not affect commensal streptococci.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2011 journal article
A facile synthesis of 1,5-disubstituted-2-aminoimidazoles: Antibiotic activity of a first generation library
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 21(15), 4516–4519.
author keywords: 2-Aminoimidazole; Amino aldehyde; Biofilm; Antibiotic
MeSH headings : Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Drug Resistance, Multiple, Bacterial / drug effects; Imidazoles / chemical synthesis; Imidazoles / chemistry; Imidazoles / pharmacology; Microbial Sensitivity Tests; Structure-Activity Relationship
TL;DR:
An efficient synthetic route to 1,5-disubstituted 2-aminoimidazoles from readily available amino acids and aldehydes has been developed and several compounds were shown to exhibit notable antibiotic activity against a variety of bacterial strains including multi-drug resistant isolates.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2011 review
Anti-biofilm compounds derived from marine sponges
[Review of ]. Marine Drugs, 9(10), 2010–2035.
Source: NC State University Libraries
Added: August 6, 2018
2011 journal article
Evaluation of 4,5-Disubstituted-2-Aminoimidazole-Triazole Conjugates for Antibiofilm/Antibiotic Resensitization Activity Against MRSA and Acinetobacter baumannii
CHEMMEDCHEM, 6(12), 2243–2251.
author keywords: aminoimidazoles; antibiotic resensitization; biofilms; MRSA; synergism
MeSH headings : Acinetobacter baumannii / drug effects; Acinetobacter baumannii / physiology; Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Biofilms / drug effects; Imidazoles / chemistry; Methicillin-Resistant Staphylococcus aureus / drug effects; Methicillin-Resistant Staphylococcus aureus / physiology; Oxacillin / chemistry; Oxacillin / pharmacology; Structure-Activity Relationship; Triazoles / chemistry
TL;DR:
This class of small molecules was found to inhibit biofilm formation by methicillin‐resistant Staphylococcus aureus (MRSA) at low‐micromolar concentrations and the ability of selected compounds to resensitize MRSA to traditional antibiotics (resensitization activity) was determined.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2011 journal article
Flustramine inspired synthesis and biological evaluation of pyrroloindoline triazole amides as novel inhibitors of bacterial biofilms
ORGANIC & BIOMOLECULAR CHEMISTRY, 9(15), 5476–5481.
MeSH headings : Amides / chemical synthesis; Amides / chemistry; Amides / pharmacology; Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Bacteria / drug effects; Biofilms / drug effects; Indole Alkaloids / chemistry; Indoles / chemical synthesis; Indoles / chemistry; Indoles / pharmacology; Inhibitory Concentration 50; Molecular Structure; Pyrroles / chemical synthesis; Pyrroles / chemistry; Pyrroles / pharmacology; Quantitative Structure-Activity Relationship; Small Molecule Libraries / chemical synthesis; Small Molecule Libraries / chemistry; Small Molecule Libraries / pharmacology
TL;DR:
Screening for the ability to modulate biofilm formation against strains of Gram-positive and Gram-negative bacteria identified several compounds with low micromolar, non-toxic IC(50) values.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2011 journal article
Growth Inhibition of Staphylococcus aureus by Mixed Monolayer Gold Nanoparticles
SMALL, 7(14), 2027–2031.
MeSH headings : Anti-Bacterial Agents / pharmacology; Gold / pharmacology; Hydrogen Bonding / drug effects; Hydrophobic and Hydrophilic Interactions / drug effects; Ligands; Metal Nanoparticles / chemistry; Microbial Sensitivity Tests; Spectrophotometry, Infrared; Staphylococcus aureus / drug effects; Staphylococcus aureus / growth & development; Sulfhydryl Compounds / pharmacology
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2011 journal article
Inhibition of Acinetobacter baumannii biofilm formation on a methacrylate polymer containing a 2-aminoimidazole subunit
Chemical Communications (Cambridge, England), 47(17), 4896–4898.
Source: NC State University Libraries
Added: August 6, 2018
2011 journal article
Intercepting Bacterial Indole Signaling with Flustramine Derivatives
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 133(50), 20160–20163.
MeSH headings : Escherichia coli / metabolism; Hydrocarbons, Brominated / metabolism; Indole Alkaloids / metabolism; Indoles / metabolism; Signal Transduction; Staphylococcus aureus / metabolism
TL;DR:
DFBr derivatives are found that are 10-1000 times more active than indole itself, demonstrating that the flustramine family of indolic natural products represent a privileged scaffold for the design of molecules to control pathogenic bacterial behavior.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2011 journal article
Synthesis and biological evaluation of 2-aminoimidazole/carbamate hybrid anti-biofilm and anti-microbial agents
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 21(4), 1257–1260.
author keywords: Biofilms; Anti-biofilm; Antibiotic; 2-Aminoimidazole; Menthyl carbamate
TL;DR:
The successful marriage of structural features from 2-aminoimidazole and menthyl carbamate classes of anti-biofilm agents has resulted in the development of a novel hybrid scaffold of biofilm modulators.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2010 journal article
A nitroenolate approach to the synthesis of 4,5-disubstituted-2-aminoimidazoles. Pilot library assembly and screening for antibiotic and antibiofilm activity
Organic & Biomolecular Chemistry, 8(12), 2814–2822.
Source: NC State University Libraries
Added: August 6, 2018
2010 journal article
Analysis of kinamycin D-mediated DNA cleavage
TETRAHEDRON LETTERS, 51(11), 1455–1458.
TL;DR:
Kinamycin D is a potent antitumor antibiotic; however the biological mode of action is poorly understood, and recent efforts suggest the natural product is capable of generating reactive oxygen species under acidic pH to induce DNA damage in the presence of a reducing agent.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2010 journal article
Chemical Synthesis and Biological Screening of 2-Aminoimidazole-Based Bacterial and Fungal Antibiofilm Agents
CHEMBIOCHEM, 11(3), 396–410.
author keywords: aminoimidazoles; biofilms; MDRAB; MRSA; multidrug-resistant bacteria
MeSH headings : Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Antifungal Agents / chemical synthesis; Antifungal Agents / chemistry; Antifungal Agents / pharmacology; Biofilms / drug effects; Drug Resistance, Multiple, Bacterial / drug effects; Imidazoles / chemical synthesis; Imidazoles / chemistry; Imidazoles / pharmacology; Microbial Sensitivity Tests
TL;DR:
This class of small molecules was found to modulate the biofilm activity of Pseudomonas aeruginosa, a multidrug‐resistant strain of Acinetobacter baumannii, a methicillin‐resistant Staphylococcus aureus strain, and the yeast Candida albicans and Cryptococcus neoformans.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2010 journal article
Identification of antibiotics using small molecule variable ligand display on gold nanoparticles
Chemical Communications (Cambridge, England), 46(40), 7516–7518.
Source: NC State University Libraries
Added: August 6, 2018
2010 journal article
Identification of aryl 2-aminoimidazoles as biofilm inhibitors in Gram-negative bacteria
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 20(12), 3797–3800.
author keywords: 2-Aminoimidazoles; Bacterial biofilms
MeSH headings : Acinetobacter baumannii / drug effects; Anti-Bacterial Agents / chemistry; Biofilms / drug effects; Escherichia coli / drug effects; Gram-Negative Bacteria / drug effects; Imidazoles / chemistry; Imidazoles / pharmacology; Plankton / drug effects; Pseudomonas aeruginosa / drug effects; Small Molecule Libraries / chemical synthesis
TL;DR:
The synthesis and biofilm inhibitory activity of a 30-member aryl amide 2-aminoimidazole library against the three biofilm forming Gram-negative bacteria Escherichia coli, Psuedomonas aeruginosa, and Acinetobacter baumannii is presented.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
14. Life Below Water
(OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2010 journal article
Modulating the development of E. coli biofilms with 2-aminoimidazoles
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 20(21), 6310–6312.
author keywords: 2-Aminoimidazoles; E. coli; Biofilms
MeSH headings : Acinetobacter baumannii / drug effects; Acinetobacter baumannii / growth & development; Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / pharmacology; Biofilms / drug effects; Drug Design; Escherichia coli / drug effects; Escherichia coli / growth & development; Hemolysis / drug effects; Humans; Imidazoles / chemical synthesis; Imidazoles / pharmacology; In Vitro Techniques; Structure-Activity Relationship
TL;DR:
The synthesis of a 20 member 2-aminoimidazole/triazole pilot library is reported, with the best inhibitor inhibiting biofilm development with an IC(50) of 13μM.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2010 journal article
Synergistic Effects between Conventional Antibiotics and 2-Aminoimidazole-Derived Antibiofilm Agents
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 54(5), 2112–2118.
MeSH headings : Acinetobacter baumannii / drug effects; Anti-Bacterial Agents / pharmacology; Bacteria / drug effects; Biofilms / drug effects; Calcium Chloride / pharmacology; Chlorides / pharmacology; Colistin / pharmacology; Drug Resistance, Bacterial; Drug Resistance, Multiple; Drug Synergism; Enterococcus faecium / drug effects; Erythrocytes / drug effects; Escherichia coli / drug effects; Humans; Imidazoles / chemistry; Imidazoles / pharmacology; Magnesium / pharmacology; Manganese Compounds / pharmacology; Methicillin-Resistant Staphylococcus aureus / drug effects; Novobiocin / pharmacology; Staphylococcus epidermidis / drug effects; Tobramycin / pharmacology; Triazoles / pharmacology
TL;DR:
The synergistic effect between a 2-aminoimidazole/triazole conjugate and antibiotics toward dispersing preestablished biofilms, culminating with a 3-orders-of-magnitude increase of biofilm dispersion toward Staphylococcus aureus biofilmms is reported.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2010 journal article
Synthesis and bacterial biofilm inhibition studies of ethyl N-(2-phenethyl) carbamate derivatives
Organic & Biomolecular Chemistry, 8(17), 3857–3859.
Source: NC State University Libraries
Added: August 6, 2018
2010 journal article
The chemical synthesis and antibiotic activity of a diverse library of 2-aminobenzimidazole small molecules against MRSA and multidrug-resistant A. baumannii
BIOORGANIC & MEDICINAL CHEMISTRY, 18(2), 663–674.
author keywords: 2-Aminobenzimidazole; Chemical library synthesis; Antibiotic; Multidrug-resistant bacteria; Staphylococcus aureus; Acinetobacter baumannii
MeSH headings : Acinetobacter baumannii / drug effects; Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Benzimidazoles / chemical synthesis; Benzimidazoles / chemistry; Benzimidazoles / pharmacology; Drug Resistance, Multiple, Bacterial; Methicillin-Resistant Staphylococcus aureus / drug effects; Microbial Sensitivity Tests; Molecular Conformation; Small Molecule Libraries; Stereoisomerism; Structure-Activity Relationship
TL;DR:
These active 2-aminobenzimidazoles retain their antibiotic activity against several strains of multidrug-resistant Staphylococcus aureus and Acinetobacter baumannii when compared to susceptible strains.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2009 journal article
A 2-Aminobenzimidazole That Inhibits and Disperses Gram-Positive Biofilms through a Zinc-Dependent Mechanism
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 131(29), 9868-+.
MeSH headings : Benzimidazoles / chemical synthesis; Benzimidazoles / chemistry; Benzimidazoles / pharmacology; Biofilms / drug effects; Biofilms / growth & development; Dose-Response Relationship, Drug; Gram-Positive Bacteria / drug effects; Magnetic Resonance Spectroscopy; Molecular Structure; Structure-Activity Relationship; Zinc / chemistry; Zinc / pharmacology
TL;DR:
Mechanistic studies showed that the activity of a lead 2-aminobenzimidazole is Zn(II)-dependent, potentially via a direct zinc-chelating mechanism.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2009 journal article
Amide Isosteres of Oroidin: Assessment of Antibiofilm Activity and C. elegans Toxicity
JOURNAL OF MEDICINAL CHEMISTRY, 52(15), 4582–4585.
MeSH headings : Amides / chemical synthesis; Amides / pharmacology; Amides / toxicity; Animals; Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / pharmacology; Biofilms / drug effects; Caenorhabditis elegans / drug effects; Pseudomonas aeruginosa / drug effects; Pseudomonas aeruginosa / physiology; Pyrroles / chemical synthesis; Pyrroles / pharmacology; Pyrroles / toxicity; Structure-Activity Relationship; Sulfonamides / chemical synthesis; Sulfonamides / pharmacology; Thiourea / chemical synthesis; Thiourea / pharmacology; Urea / chemical synthesis; Urea / pharmacology
TL;DR:
The synthesis and antibiofilm activities of sulfonamide, urea, and thiourea oroidin analogues are described and the most active derivative was able to selectively inhibit P. aeruginosa biofilm development and is also shown to be nontoxic upward of 1 mM to the development of C. elegans.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2009 journal article
Antibiofilm Activity of a Diverse Oroidin Library Generated through Reductive Acylation
JOURNAL OF ORGANIC CHEMISTRY, 74(4), 1755–1758.
MeSH headings : Acylation; Biofilms / drug effects; Oxidation-Reduction; Proteobacteria / drug effects; Pyrroles / chemical synthesis; Pyrroles / chemistry; Pyrroles / pharmacology; Small Molecule Libraries / chemical synthesis; Small Molecule Libraries / chemistry; Small Molecule Libraries / pharmacology
TL;DR:
This methodology represents a significant improvement over the generality of known methods to acylate substrates containing 2-aminoimidazoles and has the potential to have broad application to the synthesis of more advanced oroidin family members and their corresponding analogues.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
14. Life Below Water
(OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2009 review
Controlling Bacterial Biofilms
[Review of ]. CHEMBIOCHEM, 10(14), 2287–2294.
author keywords: bacteriophages; biofilms; drug discovery; natural products; quorum sensing
MeSH headings : Anti-Bacterial Agents / pharmacology; Bacteria / growth & development; Bacterial Physiological Phenomena; Bacteriophages / growth & development; Biofilms / growth & development; Biological Products / pharmacology; Drug Design; Quorum Sensing / physiology; Small Molecule Libraries
TL;DR:
The ubiquitous nature of bacteria in the environment, and the role they play in infectious disease has been one of the most extensively researched areas in biomedical science, and upwards of 75 % of microbial infections that occur in the human body are underpinned by the formation and persistence of biofilms.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2009 journal article
Evaluation of dihydrooroidin as an antifouling additive in marine paint
INTERNATIONAL BIODETERIORATION & BIODEGRADATION, 63(4), 529–532.
author keywords: Antifouling; Biofilms; Natural products
TL;DR:
Dihydrooroidin (DHO) is presented as an effective paint-based, non-cytotoxic, antifouling agent against marine biofouling processes in a marine mesocosm.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
14. Life Below Water
(OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2009 journal article
Inhibition of Acinetobacter baumannii, Staphylococcus aureus and Pseudomonas aeruginosa biofilm formation with a class of TAGE-triazole conjugates
ORGANIC & BIOMOLECULAR CHEMISTRY, 7(4), 794–802.
MeSH headings : Acinetobacter baumannii / drug effects; Anti-Bacterial Agents / chemical synthesis; Biofilms / drug effects; Imidazoles / chemistry; Pseudomonas aeruginosa / drug effects; Small Molecule Libraries / chemical synthesis; Staphylococcus aureus / drug effects; Triazoles / chemical synthesis
TL;DR:
A chemically diverse library of TAGE-triazole conjugates synthesized utilizing click chemistry on the TAGE scaffold demonstrated the most potent inhibitory effect against Staphylococcus aureus biofilm formation that has been displayed by any 2-aminoimidazole derivative.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2009 journal article
Tandem dispersion and killing of bacteria from a biofilm
ORGANIC & BIOMOLECULAR CHEMISTRY, 7(3), 603–606.
MeSH headings : Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Bacteria / drug effects; Bacteria / growth & development; Biofilms; Microbial Viability / drug effects; Photosensitizing Agents / chemistry; Photosensitizing Agents / pharmacology; Triazoles / chemistry; Triazoles / pharmacology
TL;DR:
The combined effects of biofilm dispersion with a 2-aminoimidazole-triazole conjugate and bactericidal activity with a photodynamic inactivation agent suggest a novel combination therapy for treating diverse microbial infections.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Sources: Web Of Science, NC State University Libraries
Added: August 6, 2018
2008 journal article
Construction and screening of a 2-aminoimidazole library identifies a small molecule capable of inhibiting and dispersing bacterial biofilms across order, class, and phylum
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 47(28), 5229–5231.
author keywords: biofilms; combinatorial chemistry; dispersion; inhibition; marine natural products
MeSH headings : Bacteria / drug effects; Biofilms / drug effects; Imidazoles / pharmacology; Imidazoles / therapeutic use; Small Molecule Libraries
TL;DR:
It is demonstrated that dihydrosventrin (DHS) inhibits and disperses Pseudomonas aeruginosa (multiple strains), Acinetobacter baumannii, and Bordetella bronchiseptica biofilms, making it the first small molecule reported to inhibit and disperse biofilmms across bacterial order and class through a nonbactericidal mechanism.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2008 journal article
Control of bacterial biofilms with marine alkaloid derivatives
MOLECULAR BIOSYSTEMS, 4(6), 614–621.
MeSH headings : Acinetobacter baumannii / drug effects; Acylation; Alkaloids / chemical synthesis; Alkaloids / chemistry; Alkaloids / pharmacology; Animals; Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Biofilms / drug effects; Biofilms / growth & development; Bordetella bronchiseptica / drug effects; Cell Line; Dose-Response Relationship, Drug; Imidazoles / chemical synthesis; Imidazoles / chemistry; Imidazoles / pharmacology; Mice; Microbial Sensitivity Tests; Molecular Structure; Pseudomonas aeruginosa / drug effects; Rats; Staphylococcus aureus / drug effects
TL;DR:
It is demonstrated that TAGE does not have selective toxicity against cells within the biofilm state, will inhibit biofilm development under flow conditions, indicating that the CV staining protocol correlates with the ability to be active under biomimetic conditions, and will disperse preformed P. aeruginosa biofilms.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
14. Life Below Water
(OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2008 journal article
Effects of N-pyrrole substitution on the anti-biofilm activities of oroidin derivatives against Acinetobacter baumannii
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 18(15), 4325–4327.
author keywords: biofilm; inhibition; dispersion; marine natural products; oroidin
MeSH headings : Acinetobacter baumannii / drug effects; Acinetobacter baumannii / growth & development; Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Biofilms / drug effects; Biofilms / growth & development; Humans; Imidazoles / chemistry; Microbial Sensitivity Tests; Molecular Structure; Pyrroles / chemical synthesis; Pyrroles / chemistry; Pyrroles / pharmacology; Small Molecule Libraries; Stereoisomerism; Structure-Activity Relationship
TL;DR:
This work presents the anti-biofilm activity of a small library of second generation oroidin analogues against the bacterium Acinetobacter baumannii.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
14. Life Below Water
(OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2008 journal article
Inhibition and dispersion of Pseudomonas aeruginosa biofilms with reverse amide 2-aminoimidazole oroidin analogues
ORGANIC & BIOMOLECULAR CHEMISTRY, 6(8), 1356–1363.
MeSH headings : Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Biofilms / drug effects; Biofilms / growth & development; Humans; Imidazoles / chemistry; Microbial Sensitivity Tests; Molecular Structure; Pseudomonas aeruginosa / drug effects; Pseudomonas aeruginosa / growth & development; Pyrroles / chemical synthesis; Pyrroles / chemistry; Pyrroles / pharmacology; Small Molecule Libraries; Stereoisomerism; Structure-Activity Relationship
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
14. Life Below Water
(OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2008 journal article
Inhibition and dispersion of proteobacterial biofilms
Chemical Communications (Cambridge, England), (14), 1698–1700.
Source: NC State University Libraries
Added: August 6, 2018
2008 journal article
Inhibition of HIV fusion with multivalent gold nanoparticles
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 130(22), 6896-+.
MeSH headings : Amides / chemistry; Amides / pharmacology; Gold / chemistry; Gold / pharmacology; HIV Fusion Inhibitors / chemistry; HIV Fusion Inhibitors / pharmacology; HIV Infections / drug therapy; HIV-1 / physiology; Metal Nanoparticles / chemistry; Metal Nanoparticles / therapeutic use; Quaternary Ammonium Compounds / chemistry; Quaternary Ammonium Compounds / pharmacology
TL;DR:
A fragment of the potent HIV inhibitor TAK-779 was synthesized and conjugated to 2.0 nm diameter gold nanoparticles, and the (SDC-1721)-gold nanoparticle conjugates displayed activity comparable to that of Tak-779, suggesting that multivalent presentation of small molecules on gold nanoparticle surfaces can convert inactive drugs into potent therapeutics.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science; OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2008 journal article
Kinamycin-mediated DNA cleavage under biomimetic conditions
TETRAHEDRON LETTERS, 49(19), 3157–3161.
TL;DR:
Kinamycin D has been shown to potently cleave DNA under mild biomimetic conditions and use of the endogenously abundant reductant glutathione effectively cleaved DNA in a concentration, temperature, and time-dependent fashion.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2008 journal article
Synthesis and Antibiofilm Activity of a Second-Generation Reverse-Amide Oroidin Library: A Structure-Activity Relationship Study
CHEMISTRY-A EUROPEAN JOURNAL, 14(34), 10745–10761.
author keywords: amino acids; biological activity; drug design; medicinal chemistry; structure-activity relationships
MeSH headings : Acinetobacter baumannii / drug effects; Acinetobacter baumannii / growth & development; Anti-Bacterial Agents / chemical synthesis; Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Biofilms / drug effects; Biofilms / growth & development; Drug Design; Imidazoles / chemistry; Microbial Sensitivity Tests; Molecular Structure; Pseudomonas aeruginosa / drug effects; Pseudomonas aeruginosa / growth & development; Pyrroles / chemical synthesis; Pyrroles / chemistry; Pyrroles / pharmacology; Small Molecule Libraries; Stereoisomerism; Structure-Activity Relationship
TL;DR:
A second-generation library of 2-aminoimidazole-based derivatives incorporating a "reversed amide" (RA) motif in comparison to the marine natural product oroidin were synthesized and subsequently assayed for antibiofilm activity against the medically relevant Gram-negative proteobacteria P. aeruginosa and A. baumannii.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
14. Life Below Water
(OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2008 journal article
Synthesis and screening of an oroidin library against Pseudomonas aeruginosa biofilms
CHEMBIOCHEM, 9(8), 1267–1279.
author keywords: biological activity; drug design; medicinal chemistry; natural products; structure-activity relationships
MeSH headings : Biofilms; Cross-Linking Reagents / chemistry; Databases, Factual; Drug Design; Drug Evaluation, Preclinical; Molecular Structure; Pseudomonas aeruginosa / drug effects; Pyrroles / chemical synthesis; Pyrroles / chemistry; Pyrroles / pharmacology; Structure-Activity Relationship
TL;DR:
The synthesis and determined biological activity of this unique class of compounds as inhibitors of biofilm formation that have no direct antibiotic effect are disclosed.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
14. Life Below Water
(OpenAlex)
Source: Web Of Science
Added: August 6, 2018
2008 journal article
Synthesis of a 2-aminoimidazole library for antibiofilm screening utilizing the Sonogashira reaction
JOURNAL OF ORGANIC CHEMISTRY, 73(13), 5191–5193.
MeSH headings : Anti-Bacterial Agents / chemistry; Anti-Bacterial Agents / pharmacology; Bacteria / drug effects; Biofilms / drug effects; Combinatorial Chemistry Techniques; Imidazoles / chemical synthesis; Molecular Structure
TL;DR:
The divergent synthesis of a 21-member library composed of 2-aminoimidazole compounds for evaluation as novel antibiofilm molecules is presented and the products provide adequate handles for further manipulation into more advanced analogues.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2008 journal article
Targeting RNA with cysteine-constrained peptides
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 18(2), 565–567.
author keywords: RNA; cyclic peptides; HADDOCK
MeSH headings : Base Sequence; Cysteine / chemistry; Humans; Models, Molecular; Peptides, Cyclic / chemistry; RNA / chemistry
TL;DR:
This approach has successfully identified novel cyclic peptide constructs that can target bTAR RNA and RNA/peptide interactions were effectively modeled using the HADDOCK docking program.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2007 journal article
Inhibition of Pseudomonas aeruginosa biofilm formation with bromoageliferin analogues
Journal of the American Chemical Society, 129(22), 6966-.
Source: NC State University Libraries
Added: August 6, 2018
2006 journal article
Mimicking the biological activity of diazobenzo[b]fluorene natural products with electronically tuned diazofluorene analogs
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 16(19), 5148–5151.
author keywords: kinamycins; lomaiviticins; DNA cleavage; diazofluorenes; antiproliferative activity
MeSH headings : Animals; Antineoplastic Agents / chemical synthesis; Antineoplastic Agents / pharmacology; Carbazoles / pharmacology; Cell Proliferation / drug effects; DNA Damage / drug effects; Fluorenes / chemical synthesis; Fluorenes / pharmacology; HeLa Cells; Humans; Molecular Mimicry; Structure-Activity Relationship
TL;DR:
Under appropriate electronic modulation, simple diazofluorene analogs recapitulate the DNA cleavage activity of kinamycin D under thiol-based reducing conditions, key to anticancer activity.
(via Semantic Scholar)
UN Sustainable Development Goal Categories
3. Good Health and Well-being
(Web of Science)
Source: Web Of Science
Added: August 6, 2018
2006 journal article
Tuning the oxidation properties of vanadium(V) through ligand stoichiometry
TETRAHEDRON LETTERS, 47(33), 5923–5926.
Source: Web Of Science
Added: August 6, 2018
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