Solid-phase synthesis of peptidomimetic inhibitors for the hepatitis C virus NS3 protease

Citation
Ma. Poupart et al., Solid-phase synthesis of peptidomimetic inhibitors for the hepatitis C virus NS3 protease, J ORG CHEM, 66(14), 2001, pp. 4743-4751
Citations number
35
Categorie Soggetti
Chemistry & Analysis","Organic Chemistry/Polymer Science
Journal title
JOURNAL OF ORGANIC CHEMISTRY
ISSN journal
00223263 → ACNP
Volume
66
Issue
14
Year of publication
2001
Pages
4743 - 4751
Database
ISI
SICI code
0022-3263(20010713)66:14<4743:SSOPIF>2.0.ZU;2-C
Abstract
The NS3 serine protease enzyme of the hepatitis C virus (HCV) is essential for viral replication. Short peptides mimicking the N-terminal substrate cl eavage products of the NS3 protease are known to act as weak inhibitors of the enzyme and have been used as templates for the design of peptidomimetic inhibitors. Automated solid-phase synthesis of a small library of compound s based on such a peptidomimetic scaffold has led to the identification of potent and highly selective inhibitors of the NS3 protease enzyme.