Abstract
Peptidomimetic inhibitors of general structure 1 have been prepared. Optimization of the binding affinities of these compounds through variation of the P3 hydrophobic residue is described. Selected substituted bicylic lactams displayed interesting pharmacological profiles both in vitro and in vivo.
MeSH terms
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Animals
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Crystallography, X-Ray
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Fibrinolytic Agents / chemical synthesis*
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Fibrinolytic Agents / pharmacology
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Lactams / chemical synthesis*
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Lactams / pharmacology
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Rats
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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*
Substances
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Fibrinolytic Agents
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Lactams
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Serine Proteinase Inhibitors
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Thrombin