Hepatitis C virus NS3-4A serine protease inhibitors:: Use of a P2-P1 cyclopropyl alanine combination for improved potency

被引:23
作者
Bogen, S
Saksena, AK
Arasappan, A
Gu, H
Njoroge, FG
Girijavallabhan, V
Pichardo, J
Butkiewicz, N
Prongay, A
Madison, V
机构
[1] Schering Plough Corp, Res Inst, Chem Res, Kenilworth, NJ 07033 USA
[2] Schering Plough Corp, Res Inst, Antiviral Therapy, Kenilworth, NJ 07033 USA
[3] Schering Plough Corp, Res Inst, Struct Chem, Kenilworth, NJ 07033 USA
关键词
Hepatatis C; P3 capped ketoamide; inhibitor;
D O I
10.1016/j.bmcl.2005.07.009
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Modification of the P, and P, side chains of earlier P-3-capped alpha-kctoamide inhibitor of HCV NS3 serine protease 1 resulted in the discovery of compound 24 with about 10-fold improvement in potency. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4515 / 4519
页数:5
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