Orally bioavailable small molecule ketoamide-based inhibitors of cathepsin K

被引：15

作者：

Barrett, DG

Catalano, JG

Deaton, DN ^{[1
]}

Long, ST

Miller, LR

Tavares, FX

Wells-Knecht, KJ

Wright, LL

Zhou, HQQ

机构：

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

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

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

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

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 10期

关键词：

cathepsin K; ketoamide; cysteine protease inhibitors;

D O I：

10.1016/j.bmcl.2004.02.085

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

An orally available series of ketoamide-based inhibitors of cathepsin K has been identified. Starting from a potent inhibitor with poor oral bioavailability, modifications to P-1 and P-1' elements led to enhancements in solubility and permeability. These improvements resulted in orally available cathepsin K inhibitors. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：2543 / 2546

页数：4

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