| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10591670 | Bioorganic & Medicinal Chemistry Letters | 2014 | 7 Pages |
Abstract
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.
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Authors
David Barnes-Seeman, Carri Boiselle, Christina Capacci-Daniel, Rajiv Chopra, Keith Hoffmaster, Christopher T. Jones, Mitsunori Kato, Kai Lin, Sue Ma, Guoyu Pan, Lei Shu, Jianling Wang, Leah Whiteman, Mei Xu, Rui Zheng, Jiping Fu,