Potent and selective adenosine A2A receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones

被引：19

作者：

Harris, Joel M. ^{[1
]}

Neustadt, Bernard R. ^{[1
]}

Zhang, Hongtao ^{[1
]}

Lachowicz, Jean ^{[1
]}

Cohen-Williams, Mary ^{[1
]}

Varty, Geoff ^{[1
]}

Hao, Jinsong ^{[1
]}

Stamford, Andrew W. ^{[1
]}

机构：

[1] Merck Res Labs, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 08期

关键词：

Adenosine; A(2A); A(2A) receptor; A(2A) antagonist; Adenosine receptor; Parkinson's disease; PARKINSONS-DISEASE; DISCOVERY; ISTRADEFYLLINE; DERIVATIVES;

D O I：

10.1016/j.bmcl.2011.02.045

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Antagonism of the adenosine A(2A) receptor affords a possible treatment of Parkinson's disease. In the course of investigating pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine A(2A) antagonists, we prepared [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones with potent and selective (vs A(1)) A(2A) antagonist activity. Structure-activity relationships are described for this series. (C) 2011 Elsevier Ltd. All rights reserved.

引用

收藏

页码：2497 / 2501

页数：5

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