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- Title
Click Chemistry Approach for Bis-Chromenyl Triazole Hybrids and Their Antitubercular Activity.
- Authors
Naik, Reshma J.; Kulkarni, Manohar V.; Sreedhara Ranganath Pai, K.; Nayak, Pawan G.
- Abstract
1,4-Disubstituted bis-chromenyl triazole hybrids 5a- m have been synthesized in a three-step reaction sequence from 4-(bromomethyl)-2 H-chromen-2-ones 3a- m. The intermediate azides 4a- m underwent a regioselective 1,3-dipolar cycloaddition with a 2 H-chromen-2-one linked acetylenic dipolarophile in the presence of Cu (II)/ascorbate/water/n-butanol reaction medium. Three compounds 5h- j exhibited 6.25 μg/mL MIC against M. tuberculosis. Among the compounds screened for antifungal activity, lowest MIC of 6.25 μg/mL was observed for 5c against A. 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.
- Subjects
CLICK chemistry; TRIAZOLES; ANTITUBERCULAR agents; AZIDES; MYCOBACTERIUM tuberculosis; GEL electrophoresis; ANTIFUNGAL agents; CELL-mediated cytotoxicity
- Publication
Chemical Biology & Drug Design, 2012, Vol 80, Issue 4, p516
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/j.1747-0285.2012.01441.x