Proline-based macrocyclic inhibitors of the hepatitis C virus: Stereoselective synthesis and biological activity

被引：18

作者：

Chen, KX ^{[1
]}

Njoroge, EG ^{[1
]}

Vibulbhan, B ^{[1
]}

Prongay, A ^{[1
]}

Pichardo, J ^{[1
]}

Madison, V ^{[1
]}

Buevich, A ^{[1
]}

Chan, TM ^{[1
]}

机构：

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

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2005年 / 44卷 / 43期

关键词：

antiviral agents; inhibitors; macrocycles; peptides; proteases;

D O I：

10.1002/anie.200501553

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Life-saving donut: Macrocyclization through a Mitsunobu reaction was used to synthesize a 17-membered macrocycle. The bicyclic acetal core was prepared completely diastereoselectively. The macrocyclic peptidomimetic surrogate of the P2-P3 dipeptide moiety was designed to function as a hepatitis C virus (HCV) NS3 serine protease inhibitor, and the pentapeptide α-ketoamides derived from the macrocycle were shown to be potent HCV inhibitors. (Figure Presented). © 2005 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

页码：7024 / 7028

页数：5

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