2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors

被引：13

作者：

Cai, Jiaqiang ^{[1
]}

Bennett, D. Jonathan ^{[1
]}

Rankovic, Zoran ^{[1
]}

Dempster, Maureen ^{[1
]}

Fradera, Xavier ^{[1
]}

Gillespie, Jonathan ^{[1
]}

Cumming, Iain ^{[1
]}

Finlay, William ^{[1
]}

Baugh, Mark ^{[1
]}

Boucharens, Sylviane ^{[1
]}

Bruin, John ^{[1
]}

Cameron, Kenneth S. ^{[1
]}

Hamilton, William ^{[1
]}

Kerr, Jennifer ^{[1
]}

Kinghorn, Emma ^{[1
]}

McGarry, George ^{[1
]}

Robinson, John ^{[1
]}

Scullion, Paul ^{[1
]}

Uitdehaag, Joost C. M. ^{[2
]}

van Zeeland, Mario ^{[2
]}

Potin, Dominique ^{[3
]}

Saniere, Laurent ^{[3
]}

Fouquet, Andre ^{[3
]}

Chevallier, Francois ^{[3
]}

Deronzier, Hortense ^{[3
]}

Dorleans, Cecile ^{[3
]}

Nicolai, Eric ^{[3
]}

机构：

[1] Merck Res Labs, MSD, Newhouse ML1 5SH, Lanark, Scotland

[2] Merck Res Labs, MSD, NL-5340 BH Oss, Netherlands

[3] Cerep, F-91951 Courtaboeuf, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 15期

关键词：

Cathepsin S; Transition state; Purine-6-carbonitrile; Lysosomotropism; K INHIBITORS; NEUROPATHIC PAIN; TARGET; 2-CYANO-PYRIMIDINES; DISCOVERY; REVERSAL; SCAFFOLD; SERIES;

D O I：

10.1016/j.bmcl.2010.06.049

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Starting from previously disclosed equally potent cathepsin K and S inhibitor 4-propyl-6-(3-trifluoromethylphenyl) pyrimidine-2-carbonitrile 1, a novel 2-phenyl-9H-purine-6-carbonitrile scaffold was identified to provide potent and selective cathepsin S inhibitors. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：4447 / 4450

页数：4