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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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-08, Vol.8 (16), p.2235-2240
Hauptverfasser:	Buckman, Brad O., Mohan, Raju, Koovakkat, Sunil, Liang, Amy, Lan Trinh, Morrissey, Michael M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anticoagulants - chemical synthesis Anticoagulants - chemistry Anticoagulants - pharmacology Binding Sites Biological and medical sciences Blood. Blood coagulation. Reticuloendothelial system Cattle Drug Design Factor Xa - chemistry Factor Xa Inhibitors Humans Indicators and Reagents Kinetics Medical sciences Models, Molecular Molecular Conformation Molecular Structure Pharmacology. Drug treatments Protein Conformation Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Structure-Activity Relationship Thrombin - antagonists & inhibitors Trypsin Inhibitors - chemical synthesis Trypsin Inhibitors - pharmacology
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Zusammenfassung:	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 synthesis of amidinoaryloxy 9-benzyl-8-methyl-9 H-purine, 7,8-dihydro-pteridine-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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(98)00386-2