The identification of potent, selective, and bioavailable cathepsin S inhibitors

被引：60

作者：

Gauthier, Jacques Yves

Black, W. Cameron

Courchesne, Isabelle

Cromlish, Wanda

Desmarais, Sylvie

Houle, Robert

Lamotagne, Sonia

Li, Chun Sing

Masse, Frederic

Mckay, Daniel J.

Ouellet, Marc

Robichaud, Joel

Truchon, Jean-Francois

Truong, Vouy-Linh

Wang, Qingping

Percival, M. David

机构：

[1] Merck Frosst Ctr Therapeut Res, Dept Med Chem, Kirkland, PQ H9R 4P8, Canada

[2] Biochem & Mol Biol, Kirkland, PQ H9R 4P8, Canada

[3] Mol Modeling, Kirkland, PQ H9R 4P8, Canada

[4] Comparat Med, Kirkland, PQ H9R 4P8, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 17期

关键词：

cathepsin; cathepsin S; enzyme inhibitors; trifluoroethylamine; nitrile; sulfone; antigen presentation;

D O I：

10.1016/j.bmcl.2007.06.023

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Highly potent, selective, and bioavailable inhibitors of human, mouse, or rat cathepsin S are described. The key structural features combine a sulfonyl moiety attached to a large group in P2 and a small substituent in P3. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：4929 / 4933

页数：5

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