Abstract
A new class of conformationally constrained thrombin inhibitors is described. These compounds contain a unique bicyclic pyridone scaffold which serves as a P3P2 dipeptide surrogate. The synthesis and antithrombotic activity of these inhibitors is reported.
MeSH terms
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Acetamides / chemistry*
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Acetamides / pharmacology*
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Aminopyridines / chemistry*
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Aminopyridines / pharmacology*
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Animals
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Anticoagulants / chemical synthesis
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Anticoagulants / chemistry*
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Anticoagulants / pharmacology*
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Biological Availability
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Dipeptides / chemistry
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Dogs
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Drug Design
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Drug Evaluation, Preclinical / methods
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Humans
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Molecular Mimicry
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Pyridones / chemistry
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Pyridones / pharmacology
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Rats
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Structure-Activity Relationship
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Thrombin / antagonists & inhibitors*
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Thrombosis / drug therapy
Substances
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Acetamides
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Aminopyridines
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Anticoagulants
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Dipeptides
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Pyridones
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Thrombin