953758-69-5Relevant articles and documents
Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents
Ramesh, Remya,Shingare, Rahul D.,Kumar, Vinod,Anand, Amitesh,B, Swetha,Veeraraghavan, Sridhar,Viswanadha, Srikant,Ummanni, Ramesh,Gokhale, Rajesh,Srinivasa Reddy
, p. 723 - 730 (2016)
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.