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Bioorg Med Chem Lett. 2004 Oct 4;14(19):4835-8.

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

Author information

1
Biogen Idec, Inc., Department of Medicinal Chemistry, 14 Cambridge Center, Cambridge, MA 02142, USA. chi.vu@biogenidec.com

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.

PMID:
15341934
DOI:
10.1016/j.bmcl.2004.07.048
[Indexed for MEDLINE]

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