A designed P1 cysteine mimetic for covalent and non-covalent inhibitors of HCVNS3 protease

被引：172
作者：
Narjes, F
Koehler, KF
Koch, U
Gerlach, B
Colarusso, S
Steinkuhler, C
Brunetti, M
Altamura, S
De Francesco, R
Matassa, VG
机构：
[1] IRBM, MRL Rome, Dept Chem, I-00040 Rome, Italy
[2] IRBM, MRL Rome, Dept Biochem, 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)00842-3
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The difluoromethyl group was designed by computational chemistry methods as a mimetic of the canonical P-1 cysteine thiol for inhibitors of the hepatitis C virus NS3 protease. This modification led to the development of competitive, non-covalent inhibitor 4 (K-i 30 nM) and reversible covalent inhibitors (6, K-i 0.5 nM; and 8 K-i* 10 pM). (C) 2002 Elsevier Science Ltd. All rights reserved.
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收藏
页码：701 / 704
页数：4
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