P2Y1 receptor antagonists as novel antithrombotic agents.

Abstract The P2Y 1 and P2Y 12 purinergic receptors are responsible for mediating adenosine diphosphate (ADP) dependent platelet aggregation. Evidence from P2Y 1 knockout studies as well as from nucleotide-based small molecule P2Y 1 antagonists has suggested that the antagonism of this receptor may offer a novel and effective method for the treatment of thrombotic disorders. Herein, we report the identification and optimization of a series of non-nucleotide P2Y 1 antagonists that are potent and orally bioavailable.