4.5 Article

Discovery of GS-9451: An acid inhibitor of the hepatitis C virus NS3/4A protease

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 7, Pages 2629-2634

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.01.017

Keywords

HCV; GS-9451; NS3 Protease; Solubilizing group

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The discovery of GS-9451 is reported. Modification of the P3 cap and P2 quinoline with a series of solubilizing groups led to the identification of potent HCV NS3 protease inhibitors with greatly improved pharmacokinetic properties in rats, dogs and monkeys. (C) 2012 Elsevier Ltd. All rights reserved.

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