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    6-Nitro-1-benzylquinolones exhibiting specific antitubercular activity

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    Date
    2020
    Author
    Beteck, Richard M.
    Van der Kooy, Frank
    Legoabe, Lesetja J.
    Jordaan, Audrey
    Swart, Tarryn
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    Abstract
    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
    URI
    http://hdl.handle.net/10394/35507
    https://onlinelibrary.wiley.com/doi/abs/10.1111/cbdd.13747
    https://doi.org/10.1111/cbdd.13747
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