2-(2-furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs:: Highly potent, orally active, adenosine A2A antagonists.: Part 1

被引：21

作者：

Matasi, JJ ^{[1
]}

Caldwell, JP ^{[1
]}

Zhang, HT ^{[1
]}

Fawzi, A ^{[1
]}

Cohen-Williams, ME ^{[1
]}

Varty, GB ^{[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 / 16期

关键词：

adenosine receptor; antagonist; arylindenopyrimidines;

D O I：

10.1016/j.bmcl.2005.05.086

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The structure-activity relationship of this novel class of compounds based on 2-(2-furanyl)-7-phenyl[1,2,4]-triazolo[1,5-c]pyrimidin-5-amine, 1, and its analogs was evaluated for their in vitro and in vivo adenosine A(2A) receptor antagonism. Several compounds displayed oral activity at 3 mg/kg in a rat catalepsy model. Specifically, compound 8g displayed an excellent in vitro profile, as well as a highly promising in vivo profile. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：3670 / 3674

页数：5

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