期刊
CHEMICAL BIOLOGY & DRUG DESIGN
卷 80, 期 4, 页码 516-523出版社
WILEY
DOI: 10.1111/j.1747-0285.2012.01441.x
关键词
1; 2; 3-triazole; 2H-chromen-2-one; antibacterial; antifungal; antitubercular; click reaction; cytotoxic
资金
- DST, New Delhi
1,4-Disubstituted bis-chromenyl triazole hybrids 5am have been synthesized in a three-step reaction sequence from 4-(bromomethyl)-2H-chromen-2-ones 3am. The intermediate azides 4am underwent a regioselective 1,3-dipolar cycloaddition with a 2H-chromen-2-one linked acetylenic dipolarophile in the presence of Cu (II)/ascorbate/water/n-butanol reaction medium. Three compounds 5hj exhibited 6.25 mu g/mL MIC against M.similar to tuberculosis. Among the compounds screened for antifungal activity, lowest MIC of 6.25 mu g/mL was observed for 5c against A.similar to niger that also exhibited DNA cleavage observed by agarose gel electrophoresis. All the compounds were moderately active against both Gram-positive and Gram-negative bacterial strains. The cytotoxic effect of potent compounds on normal cells (V79 and HBL100) was assessed by MTT assay.
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