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

被引：60

作者：

Poupart, MA ^{[1
]}

Cameron, DR ^{[1
]}

Chabot, C ^{[1
]}

Ghiro, E ^{[1
]}

Goudreau, N ^{[1
]}

Goulet, S ^{[1
]}

Poirier, M ^{[1
]}

Tsantrizos, YS ^{[1
]}

机构：

[1] Boehringer Ingelheim Canada Ltd, Dept Chem, Quebec City, PQ H7S 2G5, Canada

来源：

JOURNAL OF ORGANIC CHEMISTRY | 2001年 / 66卷 / 14期

关键词：

D O I：

10.1021/jo010164d

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The NS3 serine protease enzyme of the hepatitis C virus (HCV) is essential for viral replication. Short peptides mimicking the N-terminal substrate cleavage 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 compounds based on such a peptidomimetic scaffold has led to the identification of potent and highly selective inhibitors of the NS3 protease enzyme.

引用

页码：4743 / 4751

页数：9

共 35 条

[31] SOLID-PHASE SYNTHESIS OF ARYL ETHERS VIA THE MITSUNOBU REACTION
RANO, TA
CHAPMAN, KT
[J]. TETRAHEDRON LETTERS, 1995, 36 (22) : 3789 - 3792
[32] Randomised, double-blind, placebo-controlled trial of interferon α-2b with and without ribavirin for chronic hepatitis C
Reichard, O
Norkrans, G
Frydén, A
Braconier, JH
Sönnerborg, A
Weiland, O
[J]. LANCET, 1998, 351 (9096) : 83 - 87
[33] QUANTITATIVE MONITORING OF SOLID-PHASE PEPTIDE-SYNTHESIS BY THE NINHYDRIN REACTION
SARIN, VK
KENT, SBH
TAM, JP
MERRIFIELD, RB
[J]. ANALYTICAL BIOCHEMISTRY, 1981, 117 (01) : 147 - 157
[34] ON SIZE OF ACTIVE SITE IN PROTEASES .I. PAPAIN
SCHECHTER, I
BERGER, A
[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1967, 27 (02) : 157 - +
[35] Intermolecular N-alkylation of amines under conditions of the Mitsunobu reaction:: a new solid-phase synthesis of tertiary benzylamines
Zaragoza, F
Stephensen, H
[J]. TETRAHEDRON LETTERS, 2000, 41 (11) : 1841 - 1844

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