Abstract
A series of novel 8‐OMe ciprofloxacin (8‐OMe CPFX)‐1H‐1,2,3‐triazole‐isatin‐(thio) semicarbazide/oxime hybrids 6a–l with the capacity to form hydrogen bond were designed, synthesized, and evaluated for their in vitro anti‐mycobacterial activities against Mycobacterium tuberculosis (MTB) H37Rv and MDR‐TB as well as cytotoxicity. All the synthesized hybrids (MIC: 0.39–16 μg/mL) exhibited excellent activities against MTB H37Rv and MDR‐TB, and the majority of them were more potent than the parent 8‐OMe CPFX (MIC: 1.56 and 2.0 μg/mL, respectively). In particular, the most active conjugate 6h (MIC: 0.39 and 1.0 μg/mL, respectively) was two to eight times more potent in vitro than the references CPFX (MIC: 3.12 and 4.0 μg/mL, respectively) and 8‐OMe CPFX against the tested strains and was comparable with or 64‐folds more potent than RIF (MIC: 0.39 and 64 μg/mL, respectively) against MTB H37Rv and MDR‐TB, respectively. In addition, all conjugates (CC50: 16–64 μg/mL) showed acceptable cytotoxicity, although most of them were more toxic than the parent (CC50: 64 μg/mL) in VERO cell line.
Published Version
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