ChemInform Abstract: Design, Synthesis, and Biological Activity of Novel Purine and Bicyclic Pyrimidine Factor Xa Inhibitors.

B. O. BUCKMAN,R. MOHAN,S. KOOVAKKAT,A. LIANG,L. TRINH,M. M. MORRISSEY

Cheminform（2010）

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摘要

The synthesis of amidinoaryloxy 9-benzyl-8-methyl-9H-purine, 7,8-dihydropteridine-6(5H)-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.

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biological activity

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