☆ 4.5 Article

5,5′- and 6,6′-Dialkyl-5,6-dihydro-1H-pyridin-2-ones as potent inhibitors of HCV NS5B polymerase

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2009)

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Volume 19, Issue 21, Pages 6047-6052

Publisher

PERGAMON-ELSEVIER SCIENCE LTD

DOI: 10.1016/j.bmcl.2009.09.051

Keywords

Hepatitis C virus (HCV); NS5B polymerase; Small-molecule; Non-nucleoside NS5B inhibitor; 5,5 '- and 6,6 '-Dialkyl-5,6-dihydro-1H-pyridin2-ones

Categories

Chemistry, Medicinal Chemistry, Organic

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Abstract

The discovery of 5,5 '- and 6,6 '-dialkyl-5,6-dihydro-1H-pyridin-2-ones as potent inhibitors of the HCV RNA-dependent RNA polymerase (NS5B) is described. Several of these agents also display potent antiviral activity in cell culture experiments (EC50 <0.10 mu M). In vitro DMPK data for selected compounds as well as crystal structures of representative inhibitors complexed with the NS5B protein are also disclosed. (C) 2009 Elsevier Ltd. All rights reserved.

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