Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: Heterocyclic P3

被引：58

作者：

Tully, DC ^{[1
]}

Liu, H ^{[1
]}

Alper, PB ^{[1
]}

Chatterjee, AK ^{[1
]}

Epple, R ^{[1
]}

Roberts, MJ ^{[1
]}

Williams, JA ^{[1
]}

Nguyen, KT ^{[1
]}

Woodmansee, DH ^{[1
]}

Tumanut, C ^{[1
]}

Li, J ^{[1
]}

Spraggon, G ^{[1
]}

Chang, J ^{[1
]}

Tuntland, T ^{[1
]}

Harris, JL ^{[1
]}

Karanewsky, DS ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 07期

关键词：

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

D O I：

10.1016/j.bmcl.2005.12.095

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of N-alpha-2-benzoxazolyl-alpha-amino acid-(arylaminoethyl)amides were identified as potent, selective, and noncovalent inhibitors of cathepsin S. Structure-activity relationships including strategies for modulating the selectivities among cathepsins S, K, and L, and in vivo pharmacokinetics are discussed. A X-ray structure of compound 3 bound to the active site of cathepsin S is also reported. (C) 2006 Elsevier Ltd. All rights reserved.

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收藏

页码：1975 / 1980

页数：6

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