Discovery of rimonabant and its potential analogues as anti-TB drug candidates
| Title | Discovery of rimonabant and its potential analogues as anti-TB drug candidates |
| Publication Type | Journal Article |
| Year of Publication | 2015 |
| Authors | Gajbhiye, JM, More, NA, Patil, MD, Ummanni, R, Kotapalli, SS, Yogeeswari, P, Sriram, D, Masand, VH |
| Journal | Medicinal Chemistry Research |
| Volume | 24 |
| Issue | 7 |
| Pagination | 2960-2971 |
| Date Published | JUL |
| ISSN | 1054-2523 |
| Keywords | Diaryl pyrazoles, H37Rv, MTCYP-121, Mycobacterium tuberculosis, Rimonabant, tuberculosis |
| Abstract | Rimonabant and its analogues have been synthesized in moderate to good yields using a simple synthetic route. All the newly synthesized compounds were subjected to in vitro screening against M. tuberculosis and M. smegmatis. The most potent analogue JMG-14 exhibits MIC value of 3.13 compared to 3.25 and 50 A mu g/ml for ethambutol and pyrazinamide, respectively. The molecular docking reveals that pyrazole ring, number and position of halogen atoms play a crucial role in deciding interactions with MTCYP-121. These findings open up a new avenue in the search of potent anti-TB drugs with rimonabant and its novel analogue JMG-14 as lead molecules. |
| DOI | 10.1007/s00044-015-1346-4 |
| Type of Journal (Indian or Foreign) | Foreign |
| Impact Factor (IF) | 1.436 |
Divison category:
Organic Chemistry