Triamino derivatives of triazolotriazine and triazolopyrimidine as adenosine A2a receptor antagonists

被引：82

作者：

Vu, CB ^{[1
]}

Shields, P ^{[1
]}

Peng, B ^{[1
]}

Kumaravel, G ^{[1
]}

Jin, XW ^{[1
]}

Phadke, D ^{[1
]}

Wang, J ^{[1
]}

Engber, T ^{[1
]}

Ayyub, E ^{[1
]}

Petter, RC ^{[1
]}

机构：

[1] Biogen Idec Inc, Dept Med Chem, Cambridge Ctr 14, Cambridge, MA 02142 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 19期

关键词：

A(2a) antagonists; catalepsy; Parkinson's disease;

D O I：

10.1016/j.bmcl.2004.07.048

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Piperazine derivatives of 2-furanyl[1,2,4]triazolo[1,5-a][1,3,5]triazine have recently been shown to be potent and selective adenosine A(2a) receptor antagonists. We now demonstrate that potent and selective A(2a) receptor antagonists could still be obtained when the arylpiperazines are separated from the triazolotriazine core structure by an ethylenediamine spacer. Selected analogs bearing this triazolotriazine or the related triazolopyrimidine core structure have been found to be orally active in a mouse catalepsy model of Parkinson's disease. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：4835 / 4838

页数：4

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