Heterocyclic thrombin inhibitors. Part 2: quinoxalinone derivatives as novel, potent antithrombotic agents

Quinoxalinone derivatives as prototypes of dual thrombin and factor Xa inhibitors have been discovered. Nanomolar inhibition of both coagulation enzymes resulted in very potent antithrombotic activity in vitro. Quinoxalinone derivatives as prototypes of dual thrombin and factor Xa inhibitors have be...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-07, Vol.13 (14), p.2297-2302
Hauptverfasser:	Ries, Uwe J., Priepke, Henning W.M., Hauel, Norbert H., Handschuh, Sandra, Mihm, Gerhard, Stassen, Jean M., Wienen, Wolfgang, Nar, Herbert
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Blood Coagulation - drug effects Blood. Blood coagulation. Reticuloendothelial system Crystallography, X-Ray Factor Xa Inhibitors Fibrinolysin - antagonists & inhibitors Fibrinolytic Agents - chemical synthesis Fibrinolytic Agents - pharmacology Medical sciences Models, Molecular Molecular Conformation Partial Thromboplastin Time Pharmacology. Drug treatments Quinoxalines - chemical synthesis Quinoxalines - pharmacology Rats Structure-Activity Relationship Thrombin - antagonists & inhibitors Trypsin Inhibitors - chemical synthesis Trypsin Inhibitors - pharmacology
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Zusammenfassung:	Quinoxalinone derivatives as prototypes of dual thrombin and factor Xa inhibitors have been discovered. Nanomolar inhibition of both coagulation enzymes resulted in very potent antithrombotic activity in vitro. Quinoxalinone derivatives as prototypes of dual thrombin and factor Xa inhibitors have been discovered. Nanomolar inhibition of both coagulation enzymes resulted in very potent antithrombotic activity in vitro.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(03)00443-8