The discovery and synthesis of novel adenosine receptor (A2A) antagonists

被引：53

作者：

Matasi, JJ ^{[1
]}

Caldwell, JP ^{[1
]}

Hao, JS ^{[1
]}

Neustadt, B ^{[1
]}

Arik, L ^{[1
]}

Foster, CJ ^{[1
]}

Lachowicz, J ^{[1
]}

Tulshian, DB ^{[1
]}

机构：

[1] Schering Plough Res Inst, Dept Med Chem, CV & CNS, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 05期

关键词：

adenosine receptor; antagonist; arylindenopyrimidines;

D O I：

10.1016/j.bmcl.2005.01.019

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In high throughput screening of our file compounds, a novel structure 1 was identified as a potent A(2A) receptor antagonist with no selectivity over the A(1) adenosine receptor. The structure-activity relationship investigation using 1 as a template lead to identification of a novel class of compounds as potent and selective antagonists of A(2A) adenosine receptor. Compound 26 was identified to be the most potent A(2A) receptor antagonist (K-i = 0.8 nM) with 100-fold selectivity over the A(1) adenosine receptor. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：1333 / 1336

页数：4

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