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Bioorg Med Chem Lett. 2002 Nov 18;12(22):3325-8.

Capped dipeptide alpha-ketoacid inhibitors of the HCV NS3 protease.

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  • 1Department of Chemistry, IRBM, MRL Rome, Via Pontina Km 30,600, Pomezia, 00040 Rome, Italy.

Abstract

The N-terminal aminoacid of alpha-ketotripeptide inhibitors of the hepatitis C virus NS3 protease can be replaced with an alpha-hydroxy acid, leading to capped dipeptide inhibitors such as 20 with an IC(50) value of 3.0 microM. The importance of the lipophilic side chain interactions at S3 of the protease and the requirement of the capping residue with R configuration have been explained by molecular modeling studies.

PMID:
12392743
[PubMed - indexed for MEDLINE]
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