Synthesis and antiplatelet aggregation activities of prasugrel derivatives

With the metabolite of prasugrel as a lead compound,a series of 2-hydroxytetrahydrothienopyridine derivatives were designed and synthesized based on prodrug theory.Their structures were confirmed by IR,¹H NMR,¹³C NMR,MS,and HRMS.The target compounds 1-8 were biologically evaluated for their antiplatelet aggregation activity.Except for compound 5 ,most of the test compounds exhibited potent antiplatelet aggregation activity,some exhibiting similar potent activity to prasugrel.The compounds are worthy of further study to search for novel antithrombotic agents with improved potency,safety profile and chemical stability.