Potent and selective adenosine A(2A) receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones |
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| Authors: | Harris Joel M Neustadt Bernard R Zhang Hongtao Lachowicz Jean Cohen-Williams Mary Varty Geoff Hao Jinsong Stamford Andrew W |
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| Institution: | Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA |
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| Abstract: | Antagonism of the adenosine A2A receptor affords a possible treatment of Parkinson’s disease. In the course of investigating pyrazolo4,3-e]-1,2,4-triazolo1,5-c]pyrimidine A2A antagonists, we prepared 1,2,4]-triazolo4,3-c]pyrimidin-3-ones with potent and selective (vs A1) A2A antagonist activity. Structure-activity relationships are described for this series. |
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| Keywords: | Adenosine A2A A2A receptor A2A antagonist Adenosine receptor Parkinson&rsquo s disease |
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