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Potent and selective adenosine A(2A) receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones
Authors:Harris Joel M  Neustadt Bernard R  Zhang Hongtao  Lachowicz Jean  Cohen-Williams Mary  Varty Geoff  Hao Jinsong  Stamford Andrew W
Affiliation:Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA
Abstract:Antagonism of the adenosine A2A receptor affords a possible treatment of Parkinson’s disease. In the course of investigating pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine A2A antagonists, we prepared [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones with potent and selective (vs A1) A2A antagonist activity. Structure-activity relationships are described for this series.
Keywords:Adenosine   A2A   A2A receptor   A2A antagonist   Adenosine receptor   Parkinson&rsquo  s disease
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