Design of small molecule ketoamide-based inhibitors of cathepsin K

被引：27

作者：

Catalano, JG

Deaton, DN ^{[1
]}

Long, ST

McFadyen, RB

Miller, LR

Payne, JA

Wells-Knecht, KJ

Wright, LL

机构：

[1] GlaxoSmithKline, Dept Med Chem, Res Triangle Pk, NC 27709 USA

[2] GlaxoSmithKline, Dept World Wide Phys Properties, Res Triangle Pk, NC 27709 USA

[3] GlaxoSmithKline, Dept Mol Pharmacol, Res Triangle Pk, NC 27709 USA

[4] GlaxoSmithKline, Dept Res Bioanal & Drug Metab, Res Triangle Pk, NC 27709 USA

[5] GlaxoSmithKline, Discovery Res Biol, Res Triangle Pk, NC 27709 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 03期

关键词：

D O I：

10.1016/j.bmcl.2003.11.029

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of ketoamide-based inhibitors of cathepsin K has been identified. Modifications to p(2) and p(3) elements were crucial to enhancing inhibitory activity. Although not optimized, a selected inhibitor was effective in attenuating type 1 collagen hydrolysis in a surrogate assay of bone resorption. (C) 2003 Elsevier Ltd. All rights reserved.

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收藏

页码：719 / 722

页数：4

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