Design, Synthesis, and in vitro Anti-mycobacterial Evaluation of Propylene-1H-1,2,3-triazole-4-methylene-tethered (Thio)semicarbazone-isatin-moxifloxacin Hybrids

Abstract

A new class of propylene-1H-1,2,3-triazole-4-methylene-tethered (thio)semicarbazone-isatin-moxifloxacin hybrids 6a–h was designed, synthesized, and screened for their in vitro anti-mycobacterial activities against Mycobacterium tuberculosis (MTB) H37Rv and MDR-TB as well as cytotoxicity in VERO cell line. All the synthesized hybrids (MIC: 0.05–2.0 μg/mL) exhibited excellent activities against M. tuberculosis H37Rv and MDR-TB; in particular, conjugate 6c (MIC: 0.05 and 0.12 μg/mL) was no inferior to the three references MXFX (MIC: 0.10 and 0.12 μg/mL), RIF (MIC: 0.39 and 32 μg/mL), and INH (MIC: 0.05 and >128 μg/mL) against the tested two strains. All hybrids (CC50: 2–8 μg/mL) were much more cytotoxic than the parent MXFX (CC50: 128 μg/mL) should be further optimized.