Abstract
A series of dihydropyrid-2-ones was synthesized and tested for inhibitory activity against serine protease enzymes. Moderate to low nanomolar inhibitory activities were obtained against thrombin and excellent selectivity against trypsin was observed.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Cattle
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Crystallography, X-Ray
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Humans
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Models, Molecular
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Protein Binding
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Pyridones / chemical synthesis
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Pyridones / chemistry*
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Pyridones / pharmacology*
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Serine Proteinase Inhibitors / chemical synthesis
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Serine Proteinase Inhibitors / chemistry*
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Serine Proteinase Inhibitors / pharmacology*
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Thrombin / antagonists & inhibitors*
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Thrombin / chemistry
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Thrombin / metabolism*
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Trypsin / metabolism
Substances
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Pyridones
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Serine Proteinase Inhibitors
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Trypsin
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Thrombin