Potent and selective adenosine A_2A receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones

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• 作者：Joel M. Harris ; ^{joel.harris@merck.com} ; Bernard R. Neustadt ; Hongtao Zhang ; Jean Lachowicz ; Mary Cohen-Williams ; Geoff Varty ; Jinsong Hao ; Andrew W. Stamford
• 关键词：Adenosine ; A2A ; A2A receptor ; A2A antagonist ; Adenosine receptor ; Parkinson&rsquo ; s disease
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2011
• 出版时间：15 April, 2011
• 年：2011
• 卷：21
• 期：7
• 页码：2497-2501
• 全文大小：1K

文摘

Antagonism of the adenosine A_2A 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 A_2A antagonists, we prepared [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones with potent and selective (vs A₁) A_2A antagonist activity. Structure-activity relationships are described for this series.