Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives

We describe herein the discovery and development of a series of 4-arylthieno[3,2-d]pyrimidines which are potent adenosine A2A receptor antagonists. These novel compounds show high degrees of selectivity against the human A1, A2B and A3 receptor sub-types. Moreover, a number of these compounds show promising activity in vivo, suggesting potential utility in the treatment of Parkinson’s disease.

Graphical abstractThe design and synthesis of a series of biaryl thieno[3,2-d]pyrimidines is described. These novel compounds are potent adenosine A2A receptor antagonists and show high degrees of selectivity against human A1, A2B and A3 receptors. Moreover, a number of these compounds show promising activity in in vivo models of Parkinson’s disease.Figure optionsDownload full-size imageDownload as PowerPoint slide