24071-97-4Relevant articles and documents
Design and synthesis of lactam-thiophene carboxylic acids as potent hepatitis C virus polymerase inhibitors
Barnes-Seeman, David,Boiselle, Carri,Capacci-Daniel, Christina,Chopra, Rajiv,Hoffmaster, Keith,Jones, Christopher T.,Kato, Mitsunori,Lin, Kai,Ma, Sue,Pan, Guoyu,Shu, Lei,Wang, Jianling,Whiteman, Leah,Xu, Mei,Zheng, Rui,Fu, Jiping
, p. 3979 - 3985 (2014/11/08)
Herein we report the successful incorporation of a lactam as an amide replacement in the design of hepatitis C virus NS5B Site II thiophene carboxylic acid inhibitors. Optimizing potency in a replicon assay and minimizing potential risk for CYP3A4 induction led to the discovery of inhibitor 22a. This lead compound has a favorable pharmacokinetic profile in rats and dogs.