Abstract
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.
MeSH terms
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Animals
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Blood Coagulation / drug effects
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Crystallography, X-Ray
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Factor Xa Inhibitors
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Fibrinolysin / antagonists & inhibitors
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Fibrinolytic Agents / chemical synthesis*
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Fibrinolytic Agents / pharmacology*
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Models, Molecular
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Molecular Conformation
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Partial Thromboplastin Time
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Quinoxalines / chemical synthesis*
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Quinoxalines / pharmacology*
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Rats
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Structure-Activity Relationship
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Thrombin / antagonists & inhibitors*
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Trypsin Inhibitors / chemical synthesis
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Trypsin Inhibitors / pharmacology
Substances
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Factor Xa Inhibitors
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Fibrinolytic Agents
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Quinoxalines
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Trypsin Inhibitors
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Thrombin
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Fibrinolysin