288104-75-6Relevant academic research and scientific papers
Synthesis of novel 5-substituted pyrazole derivatives as cannabinoid antagonists
Alekseeva, Olga O.,Mahadevan, Anu,Wiley, Jenny L.,Martin, Billy R.,Razdan, Raj K.
, p. 2159 - 2161 (2005)
A facile seven-step sequence was developed from 4′- bromopropiophenone, utilizing a Suzuki-type coupling with an alkene, to give several novel 5-substituted pyrazole derivatives in overall yields of 11-31%. They are potent CB1 antagonists and have binding
Discovery of 2-[5-(4-chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H- pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an active metabolite. A novel, potent and selective cannabinoid-1 receptor inverse agonist with high antiobes
Wu, Chien-Huang,Hung, Ming-Shiu,Song, Jen-Shin,Yeh, Teng-Kuang,Chou, Ming-Chen,Chu, Cheng-Ming,Jan, Jiing-Jyh,Hsieh, Min-Tsang,Tseng, Shi-Liang,Chang, Chun-Ping,Hsieh, Wan-Ping,Lin, Yinchiu,Yeh, Yen-Nan,Chung, Wan-Ling,Kuo, Chun-Wei,Lin, Chin-Yu,Shy, Horng-Shing,Chao, Yu-Sheng,Shia, Kak-Shan
experimental part, p. 4496 - 4510 (2010/03/01)
By using the active metabolite 5 as an initial template, further structural modifications led to the identification of the titled compound 24 (BPR-890) as a highly potent CB1 inverse agonist possessing an excellent CB2/1 selectivity and remarkable in vivo
