Arylaminoethyl amides as noncovalent inhibitors of cathepsin S.: Part 2:: Optimization of P1 and N-aryl

被引：14

作者：

Alper, PB ^{[1
]}

Liu, H ^{[1
]}

Chatterjee, AK ^{[1
]}

Nguyen, KT ^{[1
]}

Tully, DC ^{[1
]}

Tumanut, C ^{[1
]}

Li, J ^{[1
]}

Harris, JL ^{[1
]}

Tuntland, T ^{[1
]}

Chang, J ^{[1
]}

Gordon, P ^{[1
]}

Hollenbeck, T ^{[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 / 06期

关键词：

cathepsin S; noncovalent protease inhibitor; SAR;

D O I：

10.1016/j.bmcl.2005.12.056

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A systematic study of anilines led to the discovery of a metabolically robust fluoroindoline replacement for the alkoxy aniline toxicophore in 1. Investigations of the PI pocket resulted in the discovery of a wide tolerance of functionality leading to the discovery of 11 as a potent and selective inhibitor of cathepsin S. (C) 2005 Elsevier Ltd. All rights reserved.

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收藏

页码：1486 / 1490

页数：5

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