期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 2, 页码 451-458出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.11.048
关键词
Hepatitis C virus (HCV); NS5B polymerase; Small molecule; Non-nucleoside NS5B inhibitor; 5,6-Dihydro-1H-pyridin-2-ones
5,6-Dihydro-1H-pyridin-2-one analogs were discovered as a novel class of inhibitors of genotype 1 HCV NS5B polymerase. Among these, compound 4ad displayed potent inhibitory activities in biochemical and replicon assays (IC(50) (1b) < 10 nM; IC(50) (1a) < 25 nM, EC(50) (1b) = 16 nM), good in vitro DMPK properties, as well as moderate oral bioavailability in monkeys (F = 24%). (C) 2008 Elsevier Ltd. All rights reserved.
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