Synthesis and biological evaluation of 1,2,4-triazole-3-thione and 1,3,4-oxadiazole-2-thione as anti-mycobacterial agents
| Title | Synthesis and biological evaluation of 1,2,4-triazole-3-thione and 1,3,4-oxadiazole-2-thione as anti-mycobacterial agents |
| Publication Type | Journal Article |
| Year of Publication | 2017 |
| Authors | Sonawane, A, Rode, ND, Nawale, LU, Joshi, RR, Joshi, RA, Likhite, AP, Sarkar, D |
| Journal | Chemical Biology & Drug Design |
| Volume | 90 |
| Issue | 2 |
| Pagination | 200-209 |
| Date Published | JAN |
| Type of Article | Article |
| Abstract | Resistance among dormant mycobacteria leading to multi-drug resistant (MDR) and extremely-drug resistant(XDR) tuberculosis is one of the major threats. Hence, a series of 1,2,4-triazole-3-thione and 1,3,4-oxadiazole-2-thione derivatives (4a-5c) have been synthesised and screened for their anti-tubercular activity against Mycobacterium tuberculosis H37Ra (H37Ra). Thetriazolethiones4b and 4v showed high anti-tubercular activity (both MIC and IC50) against the dormant H37Ra by in vitro and ex vivo. They were shown to have more specificity towards mycobacteria than other gram-negative and gram- positive pathogenic bacteria. The cytotoxicity was almost insignificant up to 100 μg/mL against THP-1, A549 and PANC-1 human cancer cell lines, and solubility was high in aqueous solution, indicating the potential of developing these compounds further as novel therapeutics against tuberculosis infection. |
| DOI | 10.1111/cbdd.12939 |
| Type of Journal (Indian or Foreign) | Foreign |
| Impact Factor (IF) | 1.130 |
Divison category:
Organic Chemistry