Optimization of arylindenopyrimidines as potent adenosine A2A/A1 antagonists
Bioorganic & Medicinal Chemistry Letters(2010)
摘要
Two reactive metabolites were identified in vivo for the dual A2A/A1 receptor antagonist 1. Two strategies were implemented to successfully mitigate the metabolic liabilities associated with 1. Optimization of the arylindenopyrimidines led to a number of amide, ether, and amino analogs having comparable in vitro and in vivo activity.
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关键词
A2A Antagonist,A1 Antagonist,Adenosine antagonists,Parkinson’s disease,Mouse catalepsy,Dopamine
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