Phenethyl amides as novel noncovalent inhibitors of hepatitis C virus NS3/4A protease:: Discovery, initial SAR, and molecular modeling

被引：32

作者：

Colarusso, S

Koch, U

Gerlach, B

Steinkühler, C

De Francesco, R

Altamura, S

Matassa, VG

Narjes, F

机构：

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

[2] MRL Rome, IRBM, Dept Biochem, I-00040 Pomezia, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 03期

关键词：

D O I：

10.1021/jm025594q

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The discovery of novel, reversible and competitive tripeptide inhibitors of the Hepatitis C virus NS3/4A serine protease is described. These inhibitors are characterized by the presence of a C-terminal phenethyl amide group, which extends into the prime side of the enzyme. Initial SAR together with molecular modeling and data from site-directed mutagenesis suggest an interaction of the phenethyl amide group with Lys-136.

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页码：345 / 348

页数：4

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