Works (7)

Updated: July 13th, 2023 21:16

2022 journal article

2-Aminoimidazoles Inhibit Mycobacterium abscessus Biofilms in a Zinc-Dependent Manner

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 23(6).

By: J. Belardinelli*, W. Li*, K. Martin*, M. Zeiler*, E. Lian*, C. Avanzi*, C. Wiersma*, T. Nguyen n ...

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)
Source: Web Of Science
Added: April 18, 2022

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

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
Source: Web Of Science
Added: April 22, 2019

2018 journal article

2-Aminobenzimidazoles as antibiofilm agents against Salmonella enterica serovar Typhimurium

MEDCHEMCOMM, 9(9), 1547–1552.

TL;DR: Modifications to the head, tail, and linker regions of the original hit compound elucidated new, more effective analogues that inhibit S. enterica serovar Typhimurium biofilm formation while being non-toxic to planktonic bacterial growth. (via Semantic Scholar)
UN Sustainable Development Goal Categories
2. Zero Hunger (OpenAlex)
Source: Web Of Science
Added: November 12, 2018

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).

By: A. Jeon, A. Obregon-Henao, D. Ackart, B. Podell, J. Belardinelli, M. Jackson, T. Nguyen, M. Blackledge ...

Source: NC State University Libraries
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

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

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