Design, synthesis and in vitro anti-microbial evaluation of ethylene/propylene-1H-1,2,3-triazole-4-methylene-tethered isatin-coumarin hybrids.

Design, synthesis and in vitro anti-microbial evaluation of ethylene/propylene-1H-1,2,3-triazole-4-methylene-tethered isatin-coumarin hybrids.

Curr Top Med Chem. 2017 Dec 14;:

Authors: Jin X, Xu Y, Yang X, Chen X, Wu M, Guan J, Feng L

Abstract
A new class of ethylene/propylene-1H-1,2,3-triazole-4-methylene-tethered isatin-coumarin hybrids 8a-j, integrate three anti-tuberculosis pharmacophores coumarin, isatin and 1,2,3-triazole was designed and synthesized. These hybrids were assessed for their in vitro anti-TB activity against MTB H37Rv and MDR-TB, as well as anti-bacterial activity against Gram-positive and Gram-negative strains, and cytotoxicity in VERO cell line. The results showed that all hybrids with acceptable cytotoxicity (CC50: 64-512 μg/mL) exhibited weak to moderate anti-microbial activity. The most active hybrid 8i with MIC of 50 μg/mL against MTB H37Rv and MDR-TB, also has excellent cytotoxicity profile (CC50: 128 μg/mL). The resistance index of hybrid 8i was 1, indicating hybrid 8i has no cross-resistance with the first-line anti-TB agent. Thus, hybrid 8i could act as a lead for further optimization.

PMID: 29243578 [PubMed - as supplied by publisher]

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