Works (5)

Updated: July 5th, 2023 15:47

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.

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

2015 journal article

Gold nanoparticles to improve HIV drug delivery

FUTURE MEDICINAL CHEMISTRY, 7(9), 1097–1107.

By: C. Garrido*, C. Simpson*, N. Dahl*, J. Bresee*, D. Whitehead n, E. Lindsey n, T. Harris n, C. Smith* ...

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

2014 journal article

Reversal of Mycobacterium tuberculosis phenotypic drug resistance by 2-aminoimidazole- based small molecules

PATHOGENS AND DISEASE, 70(3), 370–378.

By: D. Ackart*, E. Lindsey n, B. Podell*, R. Melander n, R. Basaraba* & C. Melander

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)
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.

By: E. Lindsey, R. Worthington, C. Alcaraz & C. Melander

Source: NC State University Libraries
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.

By: S. Rogers n, E. Lindsey n, D. Whitehead n, T. Mullikin n & C. Melander n

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
Source: Web Of Science
Added: August 6, 2018

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