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

Barnes, David and Boiselle, Carri and Chopra, Rajiv and Hoffmaster, Keith and Kato, Mitsunori and Lin, Kai and Pan, Guoyu and Zheng, Rui and Shu, Lei and Ma, Sue and Wang, Jianling and Whiteman, Leah and Xu, Mei and Fu, Jiping (2014) Design and synthesis of lactam-thiophene carboxylic acids as potent hepatitis C virus polymerase inhibitors. Bioorganic & Medicinal Chemistry Letters, 24 (16). pp. 3979-3985. ISSN 0960894X

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.

Item Type: Article
Keywords: NS5B polymerase, PXR
Date Deposited: 27 Apr 2016 23:45
Last Modified: 27 Apr 2016 23:45
URI: https://oak.novartis.com/id/eprint/21393

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