Repurposing of a drug scaffold: identification of novel sila analogues of rimonabant as potent antitubercular agents
| Title | Repurposing of a drug scaffold: identification of novel sila analogues of rimonabant as potent antitubercular agents |
| Publication Type | Journal Article |
| Year of Publication | 2016 |
| Authors | Ramesh, R, Shingare, RD, Kumar, V, Anand, A, Swetha, B, Veeraraghavan, S, Viswanadha, S, Ummanni, R, Gokhale, RS, D. Reddy, S |
| Journal | European Journal of Medicinal Chemistry |
| Volume | 122 |
| Pagination | 723-730 |
| Date Published | OCT |
| Abstract | The structural similarity between an MmpL3 inhibitor BM212, and a cannabinoid receptor modulator rimonabant, prompted us to investigate the anti-tubercular activity of rimonabant and its analogues. Further optimization, particularly through incorporation of silicon into the scaffold, resulted in new compounds with significant improvement in anti-tubercular activity against Mycobacterium tuberculosis (H37Rv). The sila analogue 18a was found to be the most potent antimycobacterial compound (MIC, 31 ng/mL) from this series with an excellent selectivity index. (C) 2016 Elsevier Masson SAS. All rights reserved. |
| DOI | 10.1016/j.ejmech.2016.07.009 |
| Type of Journal (Indian or Foreign) | Foreign |
| Impact Factor (IF) | 3.902 |
Divison category:
Biochemical Sciences