1338920-84-5Relevant articles and documents
Discovery of benzodiazepine sulfonamide-based bombesin receptor subtype 3 agonists and their unusual chirality
Liu, Ping,Lanza Jr., Thomas J.,Chioda, Marc,Jones, Carrie,Chobanian, Harry R.,Guo, Yan,Chang, Linda,Kelly, Theresa M.,Kan, Yanqing,Palyha, Oksana,Guan, Xiao-Ming,Marsh, Donald J.,Metzger, Joseph M.,Ramsay, Katie,Wang, Sheng-Ping,Strack, Alison M.,Miller, Randy,Pang, Jianmei,Lyons, Kathy,Dragovic, Jasminka,Ning, Jian G.,Schafer, Wes A.,Welch, Christopher J.,Gong, Xiaoyi,Gao, Ying-Duo,Hornak, Viktor,Ball, Richard G.,Tsou, Nancy,Reitman, Marc L.,Wyvratt, Matthew J.,Nargund, Ravi P.,Lin, Linus S.
scheme or table, p. 933 - 937 (2012/02/02)
We report herein the discovery of benzodiazepine sulfonamide-based bombesin receptor subtype 3 (BRS-3) agonists and their unusual chirality. Starting from a high-throughput screening lead, we prepared a series of BRS-3 agonists with improved potency and pharmacokinetic properties, of which compound 8a caused mechanism-based, dose-dependent food intake reduction and body weight loss after oral dosing in diet-induced obese mice. This effort also led to the discovery of a novel family of chiral molecules originated from the conformationally constrained seven-membered diazepine ring.
