Discovery of aminoquinazoline derivatives as human A2A adenosine receptor antagonists.

Novel bicyclic adenosine A2A antagonists with an aminoquinazoline moiety were designed and synthesized. The optimization of the initial lead compound based on in vitro and in vivo activity has led to the discovery of a potent and selective class of adenosine A2A antagonists. The structure–activity relationships of this novel series of bicyclic aminoquinazoline derivatives as adenosine A2A antagonists are described in detail.