期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 21, 页码 6047-6052出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.09.051
关键词
Hepatitis C virus (HCV); NS5B polymerase; Small-molecule; Non-nucleoside NS5B inhibitor; 5,5 '- and 6,6 '-Dialkyl-5,6-dihydro-1H-pyridin2-ones
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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