Title: The Role of an Amphiphilic Capping Group in Covalent and Non-Covalent Dipeptide Inhibitors of HCV NS3 Serine Protease
VOLUME: 2 ISSUE: 2
Author(s):Stefania Colarusso, Benjamin Gerlach, Claudio Giuliano, Uwe Koch, Victor G. Matassa and Frank Narjes
Affiliation:Department of Chemistry, IRBM- MRL Rome, Via Pontina km. 30.600, Pomezia, 00040 Rome, Italy.
Keywords:hcv, ns3/ns4a protease, dipeptide inhibitors
Abstract: The analysis of the S3 binding region of the Hepatitis C Virus NS3 serine protease allowed replacing the P3 amino acid of a-ketoacid tripeptide inhibitors with an amphiphilic capping group. The binding mode of α-ketoacid (8) (IC50 = 1 μM) and the role of the amphiphilic group in non-covalent phenethylamide inhibitor (15) (IC50 = 21 μM) will be discussed.
