Article
HCV NS5A replication complex inhibitors. Part 4. Optimization for genotype 1a replicon inhibitory activity.
Journal of medicinal chemistry - 13 Mar 2014
St Laurent Denis R, Serrano-Wu Michael H, Belema Makonen, Ding Min, Fang Hua, Gao Min, Goodrich Jason T, Krause Rudolph G, Lemm Julie A, Liu Mengping, Lopez Omar D, Nguyen Van N, Nower Peter T, O'Boyle Donald R, Pearce Bradley C, Romine Jeffrey L, Valera Lourdes, Sun Jin-Hua, Wang Ying-Kai, Yang Fukang, Yang Xuejie, Meanwell Nicholas A, Snyder Lawrence B
Abstract excerpt
A series of symmetrical E-stilbene prolinamides that originated from the library-synthesized lead 3 was studied with respect to HCV genotype 1a (G-1a) and genotype 1b (G-1b) replicon inhibition and selectivity against BVDV and cytotoxicity. SAR emerging from an examination of the prolinamide cap region revealed 11 to be a selective HCV NS5A inhibitor exhibiting submicromolar potency against both G-1a and G-1b...
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