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
收藏
页码：2543 / 2546
页数：4
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