Synthesis and biological activity of macrocyclic inhibitors of hepatitis C virus (HCV) NS3 protease

被引：21

作者：

Chen, KX ^{[1
]}

Njoroge, FG ^{[1
]}

Prongay, A ^{[1
]}

Pichardo, J ^{[1
]}

Madison, V ^{[1
]}

Girilavallabhan, V ^{[1
]}

机构：

[1] Schering Plough Corp, Inst Res, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 20期

关键词：

macrocycle; protease; inhibitor; hepatitis C virus;

D O I：

10.1016/j.bmcl.2005.07.033

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The 17-membered phenylalanine-based macrocycle 6 was prepared starting from 3-iodo-phenylalailine. Macrocyclization of alkene phenyl iodide 5 was effected through a palladium-catalyzed Heck reaction. The macrocyclic alpha-ketoamides were active inhibitors of the HCV NS3 protease, with the C-terminal acids and amides being more potent than tert-butyl esters. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：4475 / 4478

页数：4

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