Abstract
A new set of tetraethylene glycol tethered ciprofloxacin–isatin hybrids 5a–l with greater lipophilicity than the parent ciprofloxacin was designed, synthesized, and screened for their in vitro antimycobacterial activity against drug‐sensitive Mycobacterium tuberculosis (MTB) H37Rv and multidrug‐resistant MTB strains as well as toxicity in a mammalian VERO cell line. The preliminary results revealed that all hybrids exhibited considerable activity against MTB H37Rv with minimum inhibitory concentration in a range of 0.205–14.186 μg/mL. Especially, hybrid 5a with low cytotoxicity displayed highest activity against both drug‐sensitive MTB H37Rv and two clinically isolates multidrug‐resistant MTB strains, suggesting that it may serve as a new and promising candidate for further study.
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