Synthesis of [1,2,4]triazolo[1,5-a]pyrazines as adenosine A2A receptor antagonists

被引：24

作者：

Dowling, JE ^{[1
]}

Vessels, JT ^{[1
]}

Haque, S ^{[1
]}

Chang, HX ^{[1
]}

van Vloten, K ^{[1
]}

Kumaravel, G ^{[1
]}

Engber, T ^{[1
]}

Jin, XW ^{[1
]}

Phadke, D ^{[1
]}

Wang, J ^{[1
]}

Ayyub, M ^{[1
]}

Petter, RC ^{[1
]}

机构：

[1] Biogen Idec Inc, Cambridge, MA 02142 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 21期

关键词：

D O I：

10.1016/j.bmcl.2005.07.052

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Potent and selective antagonists of the adenosine A(2A) receptor often contain a nitrogen-rich fused-ring heterocyclic core. Replacement of the core with an isomeric ring system has previously been shown to improve target affinity, selectivity, and in vivo activity. This paper describes the preparation, by a novel route, of A(2A) receptor antagonists containing the [1,2,4]triazolo[1,5-a]pyrazine nucleus, which is isomeric with the [1,2,4]triazolo[1,5-c]pyrimidine core of a series of known A(2A) antagonists with in vivo activity in animal models of Parkinson's disease. (c) 2005 Elsevier Ltd. All rights reserved.

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收藏

页码：4809 / 4813

页数：5

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