2-Aminothiazole based P2Y1 antagonists as novel antiplatelet agents

ADP receptors, P2Y1 and P2Y12 have been recognized as potential targets for antithrombotic drugs. A series of P2Y1 antagonists that contain 2-aminothiazoles as urea surrogates were discovered. Extensive SAR of the thiazole ring is described. The most potent compound 7j showed good P2Y1 binding (Ki = 12 nM), moderate antagonism of platelet aggregation (PA IC50 = 5.2 μM) and acceptable PK in rats.