Dipeptide nitrile inhibitors of cathepsin K

被引：22

作者：

Altmann, E ^{[1
]}

Aichholz, R ^{[1
]}

Betschart, C ^{[1
]}

Buhl, T ^{[1
]}

Green, J ^{[1
]}

Lattmann, R ^{[1
]}

Missbach, M ^{[1
]}

机构：

[1] Novartis Inst Biomed Res, CH-4002 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 09期

关键词：

D O I：

10.1016/j.bmcl.2006.01.104

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of dipeptidyl nitrites as inhibitors of cathepsin K have been explored starting from lead structure 1 (Cbz-Leu-NH-CH2-CN IC50 = 39 nM). Attachment of non-natural amino acid side chains in P1 and modification of the P3 subunit led to inhibitors with higher potency and improved pharmacokinetic properties. (C) 2006 Elsevier Ltd. All rights reserved.

引用

页码：2549 / 2554

页数：6

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