953758-69-5Relevant academic research and scientific papers
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.
Design, synthesis and biological evaluation of CB1 cannabinoid receptor ligands derived from the 1,5-diarylpyrazole scaffold
Tu, Guogang,Xiong, Fang,Huang, Huiming,Kuang, Binhai,Li, Shaohua
, p. 222 - 230 (2011/11/06)
The CB1 receptor belongs to the G-protein-coupled receptor superfamily. CB1 antagonism has been considered as a new therapeutic target for the treatment of obesity. In this study, we report the synthesis and in vitro binding affinity assay of some 1,5-dia
