Beteck, Richard M.Van der Kooy, FrankLegoabe, Lesetja J.Jordaan, AudreySwart, Tarryn2020-08-062020-08-062020Beteck, R.M. et al. 2020. 6-Nitro-1-benzylquinolones exhibiting specific antitubercular activity. Chemical biology & drug design, (In press). [https://doi.org/10.1111/cbdd.13747]1747-02771747-0285 (Online)http://hdl.handle.net/10394/35507https://onlinelibrary.wiley.com/doi/abs/10.1111/cbdd.13747https://doi.org/10.1111/cbdd.13747In 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 (MIC90 ˂ 0.24 µm ) against MTB. 8e , however, showed no activity against DprE1 mutant, suggesting DprE1 as the likely target for this compound classenDprE1 enzymeMycobacterium tuberculosisNitro drugsQuinolonesArticle