443141-90-0Relevant 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 (2016/08/04)
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.
Pentacycle derivatives as cannabinoid CB1 receptor ligands
Lee, Suk Ho,Seo, Hee Jeong,Kim, Min Ju,Kang, Suk Youn,Lee, Sung-Han,Ahn, Kwangwoo,Lee, MinWoo,Han, Ho-Kyun,Kim, Jeongmin,Lee, Jinhwa
scheme or table, p. 6632 - 6636 (2010/06/12)
Cannabinoid CB-1 receptors have been the focus of extensive studies since the first clinical results of rimonabant (SR141716) for the treatment of obesity and obesity-related metabolic disorders were reported in 2001. To further evaluate the properties of
Biarylpyrazolyl oxadiazole as potent, selective, orally bioavailable cannabinoid-1 receptor antagonists for the treatment of obesity
Suk, Ho Lee,Hee, Jeong Seo,Lee, Sung-Han,Myung, Eun Jung,Park, Ji-Hyun,Park, Hyun-Ju,Yoo, Jakyung,Yun, Hoseop,Na, Jooran,Suk, Youn Kang,Song, Kwang-Seop,Kim, Min-Ah,Chang, Chong-Hwan,Kim, Jeongmin,Lee, Jinhwa
body text, p. 7216 - 7233 (2009/11/30)
Since the CB1 cannabinoid receptor antagonist 1 (SR141716, rimonabant) was previously reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target for the treatment of obesity. In the present study, biarylpyrazole analo