Exploration of the P1SAR of aldehyde cathepsin K inhibitors

被引：43

作者：

Catalano, JG

Deaton, DN

Furfine, ES

Hassell, AM

McFadyen, RB

Miller, AB

Miller, LR

Shewchuk, LM

Willard, DH

Wright, LL

机构：

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

[2] GlaxoSmithKline, Dept Mol Biol, Res Triangle Pk, NC 27709 USA

[3] GlaxoSmithKline, Dept Struct Chem, Res Triangle Pk, NC 27709 USA

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

[5] GlaxoSmithKline, Dept Gene Express & Prot Biochem, Res Triangle Pk, NC 27709 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 01期

关键词：

D O I：

10.1016/j.bmcl.2003.09.088

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S-1 subsite with a series of alpha-amino aldehyde derivatives substituted at the P-1 position afforded compounds with cathepsin K IC(50)s between 52 muM and 15 nM. (C) 2003 Elsevier Ltd. All rights reserved.

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收藏

页码：275 / 278

页数：4

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