Author/Authors :
Jeffrey A. Pfefferkorn، نويسنده , , Chulho Choi، نويسنده , , Thomas Winters، نويسنده , , Robert Kennedy، نويسنده , , Liguo Chi، نويسنده , , Lisa A. Perrin، نويسنده , , Gina Lu، نويسنده , , Yun-Wen Ping، نويسنده , , Tom McClanahan، نويسنده , , Richard Schroeder، نويسنده , , Michael T. Leininger، نويسنده , , Andrew Geyer، نويسنده , , Sabine Schefzick، نويسنده , , James Atherton، نويسنده ,
Abstract :
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.
Keywords :
P2Y1 receptor , GPCR antagonist , antiplatelet , cardiovascular disease , antithrombotic
