Design and synthesis of lactam-thiophene carboxylic acids as potent hepatitis C virus polymerase inhibitors

DOI: 10.1016/j.bmcl.2014.06.031

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 3979 - 3985 (2014)

Update date:2022-07-29

Topics:

Authors:

Barnes-Seeman, David

Boiselle, Carri

Capacci-Daniel, Christina

Chopra, Rajiv

Hoffmaster, Keith

Jones, Christopher T.

Kato, Mitsunori

Lin, Kai

Ma, Sue Ma, Sue

Pan, Guoyu

Shu, Lei

Wang, Jianling

Whiteman, Leah

Xu, Mei Xu, Mei

Zheng, Rui

Fu, Jiping

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Article abstract of DOI:10.1016/j.bmcl.2014.06.031

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.

Full text of DOI:10.1016/j.bmcl.2014.06.031

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