Investigation of ketone warheads as alternatives to the nitrile for preparation of potent and selective cathepsin K inhibitors

被引：23

作者：

Boyd, Michael J. ^{[1
]}

Crane, Sheldon N. ^{[1
]}

Robichaud, Joel ^{[1
]}

Scheigetz, John ^{[1
]}

Black, W. Cameron ^{[1
]}

Chauret, Nathalie ^{[1
]}

Wang, Qingping ^{[1
]}

Masse, Frederic ^{[1
]}

Oballa, Renata M. ^{[1
]}

机构：

[1] Merck Frosst Ctr Therapeut Res, Pointe Claire, PQ H9R 4P8, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 03期

关键词：

Cathepsin K; Ketone; Odanacatib; DESIGN;

D O I：

10.1016/j.bmcl.2008.12.053

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Amino ketone warheads were explored as alternatives to the nitrile group of a potent and selective cathepsin K inhibitor. The resulting compounds were potent and selective inhibitors of cathepsin K and these nitrile replacements had a significant effect on metabolism and pharmacokinetics. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：675 / 679

页数：5

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