Exploration of the P2-P3SAR of aldehyde cathepsin K inhibitors

被引：21

作者：

Boros, EE

Deaton, DN

Hassell, AM

McFadyen, RB

Miller, AB

Miller, LR

Paulick, MG

Shewchuk, LM

Thompson, JB

Willard, DH

Wright, LL

机构：

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

[2] GlaxoSmithKline, Discovery Res, Computat Analyt & Struct Sci, Res Triangle Pk, NC 27709 USA

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

[4] GlaxoSmithKline, Dept Gene Express & Prot Biochem, 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 / 13期

关键词：

D O I：

10.1016/j.bmcl.2004.04.084

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-2 and S-3 subsites with a series of carbamate derivatized norleucine aldehydes substituted at the P-2 and P-3 positions afforded analogs with cathepsin K IC(50)s between 600 nM and 130 pM. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：3425 / 3429

页数：5

共 22 条

[1] PREPARATION AND REACTIONS OF FUNCTIONALIZED BENZYLIC ORGANOMETALLICS OF ZINC AND COPPER [J].