Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors

Abstract The synthesis of amidinoaryloxy 9-benzyl-8-methyl-9 H -purine, 7,8-dihydropteridine-6(5 H )-one and 5,7-dihydropyrimido[4,5- b ][1,4]oxazine-6-one inhibitors of Factor Xa is described. These compounds show nanomolar potency against FXa and maintain high selectivity over thrombin and trypsin.