Click chemistry approach for bis-chromenyl triazole hybrids and their antitubercular activity
Naik, RJ; Kulkarni, MV; Sreedhara Ranganath Pai, K; Nayak, PG
HERO ID
1454836
Reference Type
Journal Article
Year
2012
Language
English
PMID
| HERO ID | 1454836 |
|---|---|
| In Press | No |
| Year | 2012 |
| Title | Click chemistry approach for bis-chromenyl triazole hybrids and their antitubercular activity |
| Authors | Naik, RJ; Kulkarni, MV; Sreedhara Ranganath Pai, K; Nayak, PG |
| Journal | Chemical Biology and Drug Design |
| Volume | 80 |
| Issue | 4 |
| Page Numbers | 516-523 |
| Abstract | 1,4-Disubstituted bis-chromenyl triazole hybrids 5a-m have been synthesized in a three-step reaction sequence from 4-(bromomethyl)-2H-chromen-2-ones 3a-m. The intermediate azides 4a-m 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 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. |
| Doi | 10.1111/j.1747-0285.2012.01441.x |
| Pmid | 22737986 |
| Wosid | WOS:000308994500003 |
| Is Certified Translation | No |
| Dupe Override | No |
| Is Public | Yes |
| Language Text | English |
| Keyword | 1; 2; 3-triazole; 2H-chromen-2-one; antibacterial; antifungal; antitubercular; click reaction; cytotoxic |