Design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part I

被引：20

作者：

Liu, H ^{[1
]}

Tully, DC ^{[1
]}

Epple, R ^{[1
]}

Bursulaya, B ^{[1
]}

Li, J ^{[1
]}

Harris, JL ^{[1
]}

Williams, JA ^{[1
]}

Russo, R ^{[1
]}

Tumanut, C ^{[1
]}

Roberts, MJ ^{[1
]}

Alper, PB ^{[1
]}

He, Y ^{[1
]}

Karanewsky, DS ^{[1
]}

机构：

[1] Genom Inst Novartis Res Fdn, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 22期

关键词：

cathepsin S; cathepsin; cysteine protease inhibitor; peptidomimetics; noncovalent inhibitors;

D O I：

10.1016/j.bmcl.2005.08.017

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of N-alpha-acyl-alpha-amino acid-(arylaminoethyl)amides were found to be potent and noncovalent cathepsin S inhibitors. Compound 20 possessed high cathepsin S affinity (K-i = 3.3 nM) and showed excellent selectivity over cathepsin K, L, F, and V. Molecular modeling, design, synthesis, and in vitro activity are described. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：4979 / 4984

页数：6

共 28 条

[1] Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors [J].