Methylene amine substituted arylindenopyrimidines as potent adenosine A_2A/A₁ antagonists

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• 作者：Brian C. Shook ; Stefanie Rassnick ; Daniel Hall ; Kenneth C. Rupert ; Geoffrey R. Heintzelman ; Kristen Hansen ; Devraj Chakravarty ; James L. Bullington ; Robert H. Scannevin ; Brian Magliaro ; Lori Westover
• 关键词：A_2A antagonists ; A₁ antagonists ; Adenosine antagonists ; Parkinson’ ; s disease ; Catalepsy ; Dopamine
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：1 May 2010
• 年：2010
• 卷：20
• 期：9
• 页码：2864-2867
• 全文大小：1949 K

文摘

A novel series of arylindenopyrimidines were identified as A_2A and A₁ receptor antagonists. The series was optimized for in vitro activity by substituting the 8- and 9-positions with methylene amine substituents. The compounds show excellent activity in mouse models of Parkinson’s disease when dosed orally.