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Design, Synthesis, and in vitro Anti‐mycobacterial Evaluation of Propylene‐1 H ‐1,2,3‐triazole‐4‐methylene‐tethered (Thio)semicarbazone‐isatin‐moxifloxacin Hybrids
Author(s) -
Xu Zhi,
Song XuFeng,
Fan Jing,
Lv ZaoSheng
Publication year - 2018
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3004
Subject(s) - chemistry , isatin , thio , in vitro , moxifloxacin , triazole , semicarbazone , mycobacterium tuberculosis , vero cell , methylene , stereochemistry , tuberculosis , organic chemistry , biochemistry , antibiotics , medicine , pathology
A new class of propylene‐1 H ‐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) H 37 Rv 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 H 37 Rv 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 (CC 50 : 2–8 μg/mL) were much more cytotoxic than the parent MXFX (CC 50 : 128 μg/mL) should be further optimized.