Methylene amine substituted arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.

Abstract A novel series of arylindenopyrimidines were identified as A 2A and A 1 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.