Literature

Abstract

Reversible tetrapeptide-based compounds have been shown to effectively inhibit the hepatitis C virus NS3.4A protease. Inhibition of viral replicon RNA production in Huh-7 cells has also been demonstrated. We show herein that the inclusion of hydrogen bond donors on the P4 capping group of tetrapeptide-based inhibitors result in increased binding potency to the NS3.4A protease. The capping groups also impart significant effects on the pharmacokinetic profile of these inhibitors.

DOI： 10.1016/j.bmcl.2007.03.090

Inhibitors of hepatitis C virus NS3·4A protease. Effect of P4 capping groups on inhibitory potency and pharmacokinetics

Bioorganic & Medicinal Chemistry Letters 2007.0

Novel Peptidomimetic Hepatitis C Virus NS3/4A Protease Inhibitors Spanning the P2–P1′ Region

ACS Medicinal Chemistry Letters 2014.0

Synthesis and antiviral activity of novel HCV NS3 protease inhibitors with P4 capping groups

Bioorganic & Medicinal Chemistry Letters 2012.0

Inhibitors of hepatitis C virus NS3/4A: α-Ketoamide based macrocyclic inhibitors

Bioorganic & Medicinal Chemistry Letters 2009.0

Discovery of a series of novel compounds with moderate anti-hepatitis C virus NS3 protease activity in vitro

Bioorganic & Medicinal Chemistry 2015.0

Achiral Pyrazinone-Based Inhibitors of the Hepatitis C Virus NS3 Protease and Drug-Resistant Variants with Elongated Substituents Directed Toward the S2 Pocket