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

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. The synthe...

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