Article
Hepatitis C virus NS5A replication complex inhibitors. Part 6: Discovery of a novel and highly potent biarylimidazole chemotype with inhibitory activity toward genotypes 1a and 1b replicons.
Journal of medicinal chemistry - 13 Mar 2014
Belema Makonen, Nguyen Van N, Romine Jeffrey L, St Laurent Denis R, Lopez Omar D, Goodrich Jason T, Nower Peter T, O'Boyle Donald R, Lemm Julie A, Fridell Robert A, Gao Min, Fang Hua, Krause Rudolph G, Wang Ying-Kai, Oliver A Jayne, Good Andrew C, Knipe Jay O, Meanwell Nicholas A, Snyder Lawrence B
Abstract excerpt
A medicinal chemistry campaign that was conducted to address a potential genotoxic liability associated with an aniline-derived scaffold in a series of HCV NS5A inhibitors with dual GT-1a/-1b inhibitory activity is described. Anilides 3b and 3c were used as vehicles to explore structural modifications that retained antiviral potency while removing the potential for metabolism-based unmasking of the embedded...
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