Premium
6‐Nitro‐1‐benzylquinolones exhibiting specific antitubercular activity
Author(s) -
Beteck Richard M.,
Jordaan Audrey,
Swart Tarryn,
Van Der Kooy Frank,
Warner Digby F.,
Hoppe Heinrich C.,
Legoabe Lesetja J.
Publication year - 2020
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13747
Subject(s) - acinetobacter baumannii , microbiology and biotechnology , pseudomonas aeruginosa , staphylococcus aureus , klebsiella pneumonia , mycobacterium tuberculosis , enterobacter aerogenes , escherichia coli , antibacterial activity , cytotoxicity , chemistry , biology , in vitro , bacteria , tuberculosis , medicine , biochemistry , genetics , pathology , gene
In this study, we synthesized novel nitro quinolone‐based compounds and tested them in vitro against a panel of Gram‐positive and Gram‐negative pathogens including Mycobacterium tuberculosis (MTB), Pseudomonas aeruginosa , Acinetobacter baumannii , Klebsiella pneumonia , Staphylococcus aureus , and Escherichia coli for antibacterial activities and also against HeLa cells for overt cytotoxicity. Compound 8e was identified as a non‐toxic, potent hit with selective activity (MIC 90 ˂ 0.24 µ m ) against MTB. 8e , however, showed no activity against DprE1 mutant, suggesting DprE1 as the likely target for this compound class.