Evolution, synthesis and SAR of tripeptide α-ketoacid inhibitors of the hepatitis C virus NS3/NS4A serine protease

被引：47

作者：

Colarusso, S ^{[1
]}

Gerlach, B ^{[1
]}

Koch, U ^{[1
]}

Muraglia, E ^{[1
]}

Conte, I ^{[1
]}

Stansfield, I ^{[1
]}

Matassa, VG ^{[1
]}

Narjes, F ^{[1
]}

机构：

[1] IRBM, Dept Chem, MRL Rome, I-00040 Rome, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(01)00843-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

N-Terminal truncation of the hexapeptide ketoacid I gave rise to potent tripeptide inhibitors of the hepatitis C virus NS3 protcase/NS4A cofactor complex. Optimization of these tripeptides led to ketoacid 30 with an IC50 of 0.38 muM. The SAR of these tripeptides is discussed in the light of the recently published crystal Structures of a ternary tripetide/NS3/NS4A complexes. (C) 2002 Elsevier Science Ltd. All rights reserved.

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页码：705 / 708

页数：4

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