Ramesh, Remya ; Shingare, Rahul D. ; Kumar, Vinod ; Anand, Amitesh ; B, Swetha ; Veeraraghavan, Sridhar ; Viswanadha, Srikant ; Ummanni, Ramesh ; Gokhale, Rajesh ; Srinivasa Reddy, D. (2016) Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents European Journal of Medicinal Chemistry, 122 . pp. 723-730. ISSN 0223-5234
Full text not available from this repository.
Official URL: http://doi.org/10.1016/j.ejmech.2016.07.009
Related URL: http://dx.doi.org/10.1016/j.ejmech.2016.07.009
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.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to National Library of Medicine |
| ID Code: | 121935 |
| Deposited On: | 23 Jul 2021 08:44 |
| Last Modified: | 30 Jul 2021 07:42 |
Repository Staff Only: item control page
