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6-Nitro-1-benzylquinolones exhibiting specific antitubercular activity

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Wiley

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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 (MIC90 ˂ 0.24 µm ) against MTB. 8e , however, showed no activity against DprE1 mutant, suggesting DprE1 as the likely target for this compound class

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Beteck, 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]

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