Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists

A series of N-pyrimidinyl-2-phenoxyacetamide adenosine A2A antagonists is described. SAR studies led to compound 14 with excellent potency (Ki = 0.4 nM), selectivity (A1/A2A > 100), and efficacy (MED 10 mg/kg po) in the rat haloperidol-induced catalepsy model for Parkinson’s disease.

A series of N-pyrimidinyl-2-phenoxyacetamide adenosine A2A antagonists is described. SAR studies led to compound 14 with excellent potency, selectivity, and efficacy in the rat haloperidol-induced catalepsy model for Parkinson’s disease.Figure optionsDownload as PowerPoint slide