2-Aminothiazole based P2Y1 antagonists as novel antiplatelet agents

Abstract ADP receptors, P2Y 1 and P2Y 12 have been recognized as potential targets for antithrombotic drugs. A series of P2Y 1 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 P2Y 1 binding ( K i  = 12 nM), moderate antagonism of platelet aggregation (PA IC 50  = 5.2 μM) and acceptable PK in rats.