Works (5)

Updated: July 7th, 2023 21:18

2019 journal article

Identification of Anti-Mycobacterial Biofilm Agents Based on the 2-Aminoimidazole Scaffold

CHEMMEDCHEM, 14(9), 927–937.

By: T. Nguyen n, B. Minrovic*, R. Melander* & C. Melander

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


By: S. Martin*, R. Melander*, C. Brackett n, A. Scott*, C. Chandler*, C. Nguyen n, B. Minrovic*, S. Harrill n ...

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)
Source: Web Of Science
Added: August 5, 2019

2019 journal article

Using Small-Molecule Adjuvants to Repurpose Azithromycin for Use against Pseudomonas aeruginosa


By: V. Hubble*, B. Hubbard n, B. Minrovic*, R. Melander* & C. Melander

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)
Source: Web Of Science
Added: April 20, 2020

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.


By: M. Milton*, B. Minrovic n, D. Harris*, B. Kang*, D. Jung*, C. Lewis n, R. Thompson*, R. Melander n ...

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)
Source: Web Of Science
Added: January 28, 2019

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


By: T. Nguyen n, M. Blackledge*, E. Lindsey n, B. Minrovic n, D. Ackart*, A. Jeon*, A. Obregon-Henao*, R. Melander n, R. Basaraba*, C. Melander

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

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