1311150-23-8Relevant articles and documents
SAR studies on a series of N-benzyl-4-heteroaryl-1-(phenylsulfonyl) piperazine-2-carboxamides: Potent inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus
Gentles, Robert G.,Ding, Min,Zheng, Xiaofan,Chupak, Louis,Poss, Michael A.,Beno, Brett R.,Pelosi, Lenore,Liu, Mengping,Lemm, Julie,Wang, Ying-Kai,Roberts, Susan,Gao, Min,Kadow, John
scheme or table, p. 3142 - 3147 (2011/06/24)
Described herein is the initial optimization of (+/-) N-benzyl-4- heteroaryl-1-(phenylsulfonyl)piperazine-2-carboxamide (1), a hit discovered in a high throughput screen run against the NS5B polymerase enzyme of the hepatitis C virus. This effort resulted in the identification of (S)-N-sec-butyl-6-((R)-3- (4-(trifluoromethoxy)benzylcarbamoyl)-4-(4-(trifluoromethoxy)phenylsulfonyl) piperazin-1-yl)pyridazine-3-carboxamide (2), that displayed potent replicon activities against HCV genotypes 1b and 1a (EC50 1b/1a = 7/89 nM).