Abstract
A series of noncovalent tripeptidic thrombin inhibitors incorporating a unidazolylethynyl moiety at P1 was investigated. A number of compounds of this series were highly potent and selective versus trypsin, and several compounds demonstrated good oral absorption in rats (F = 58% for compound 19).
MeSH terms
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Acetylene / chemical synthesis
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Acetylene / pharmacology
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Alkynes / chemical synthesis
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Alkynes / metabolism*
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Animals
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Cattle
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Hemostatics / antagonists & inhibitors
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Hemostatics / metabolism
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Humans
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Imidazoles / chemical synthesis
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Imidazoles / metabolism*
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Imidazoles / pharmacology*
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Models, Molecular
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Protein Binding
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Serine Proteinase Inhibitors / chemical synthesis*
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Serine Proteinase Inhibitors / pharmacology
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Structure-Activity Relationship
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Thrombin / antagonists & inhibitors*
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Thrombin / metabolism
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Trypsin / metabolism
Substances
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Alkynes
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Hemostatics
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Imidazoles
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Serine Proteinase Inhibitors
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Trypsin
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Thrombin
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Acetylene