2,6-Diaryl-4-phenacylaminopyrimidines as potent and selective adenosine A2A antagonists with reduced hERG liability

Bioorganic & Medicinal Chemistry Letters（2008）

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摘要

Pyrimidine-based adenosine A2A antagonists were explored to attenuate hERG while improving A1 selectivity. Replacement of the basic amine side chain led to potent and selective A2A antagonists, with reduced hERG liability.

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关键词

A2A antagonists,Adenosine receptor,Parkinson’s disease,Phenacylaminopyrimidines,hERG

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