P2Y1 receptor antagonists as novel antithrombotic agents

The P2Y1 and P2Y12 purinergic receptors are responsible for mediating adenosine diphosphate (ADP) dependent platelet aggregation. Evidence from P2Y1 knockout studies as well as from nucleotide-based small molecule P2Y1 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 P2Y1 antagonists that are potent and orally bioavailable.

This manuscript describes the synthesis and evaluation of a series of P2Y1 receptor antagonists for the treatment of platelet aggregation disorders.Figure optionsDownload as PowerPoint slide