N-arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B

被引：30

作者：

Greenspan, PD ^{[1
]}

Clark, KL ^{[1
]}

Cowen, SD ^{[1
]}

McQuire, LW ^{[1
]}

Tommasi, RA ^{[1
]}

Farley, DL ^{[1
]}

Quadros, E ^{[1
]}

Coppa, DE ^{[1
]}

Du, ZM ^{[1
]}

Fang, Z ^{[1
]}

Zhou, HH ^{[1
]}

Doughty, J ^{[1
]}

Toscano, KT ^{[1
]}

Wigg, AM ^{[1
]}

Zhou, SY ^{[1
]}

机构：

[1] Novartis Inst Biomed Res, E Hanover, NJ 07936 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 22期

关键词：

D O I：

10.1016/j.bmcl.2003.08.006

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

To improve the pharmacokinetics of a previously reported series of dipeptidyl nitrile cathepsin B inhibitors, the P-2-P-3 amide group was replaced with an arylamine. Further optimization of this template resulted in highly potent and selective inhibitors with excellent oral availability. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：4121 / 4124

页数：4

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