Ciprofloxacin-isatin-1H-1,2,3-triazole Hybrids: Design, Synthesis, and in vitro Anti-tubercular Activity against M. tuberculosis

Abstract

A new set of ciprofloxacin (CPFX)-isatin-1H-1,2,3-triazole hybrids 6a–l with greater lipophilicity compared with the parent CPFX was designed, synthesized, and assessed for their in vitro anti-mycobacterial activity against Mycobacterium tuberculosis (MTB) H37Rv as well as cytotoxicity in VERO cell line. The preliminary results showed that all hybrids (MIC: 0.39–50 μg/mL) exhibited promising activities against MTB H37Rv, and six of them (MIC: 0.39–1.56 μg/mL) were more active than the parent CPFX (MIC: 3.12 μg/mL). In particular, the most active conjugate 6h (MIC: 0.39 μg/mL) was comparable with RIF (MIC: 0.39 μg/mL), and eight times more potent than CPFX. All conjugates (CC50: 4–64 μg/mL) were more toxic than the parent (CC50: 128 μg/mL) in VERO cell lines, and the most active hybrids, which also displayed the highest cytotoxicity, should be further optimized.