Bioorganic & Medicinal Chemistry Letters 2004-10-04

Triamino derivatives of triazolotriazine and triazolopyrimidine as adenosine A2a receptor antagonists.

Chi B Vu, Pamela Shields, Bo Peng, Gnanasambandam Kumaravel, Xiaowei Jin, Deepali Phadke, Joy Wang, Thomas Engber, Eman Ayyub, Russell C Petter

Index: Bioorg. Med. Chem. Lett. 14(19) , 4835-8, (2004)

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Abstract

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.