Potent and selective adenosine A_2A receptor antagonists: 1,2,4-Triazolo[1,5-c

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• 作者：Bernard R. Neustadt ; Hong Liu ; Jinsong Hao ; William J. Greenlee ; Andrew W. Stamford ; Carolyn Foster ; Leyla Arik ; Jean Lachowicz ; Hongtao Zhang ; Rosalia Bertorelli ; Silva Fredduzzi ; Geoffrey Varty ; Mar
• 关键词：Adenosine A_2a ; Parkinson’ ; s disease ; 1 ; 2 ; 4-Triazolo[1 ; 5-c]pyrimidine
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 出版时间：1 February 2009
• 年：2009
• 卷：19
• 期：3
• 页码：967-971
• 全文大小：199 K

文摘

Antagonism of the adenosine A_2a receptor offers great promise in the treatment of Parkinson’s disease. In the course of exploring pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine A_2A antagonists, which led to clinical candidate SCH 420814, we prepared 1,2,4-triazolo[1,5-c]pyrimidines with potent and selective (vs A₁) A_2a antagonist activity, including oral activity in the rat haloperidol-induced catalepsy model. Structure–activity relationships and plasma levels are described for this series.