Abstract
The synthesis and activity of novel benzothiophene derivatives are described. In the t-Pa-induced fibrin clot lysis assay, several compounds inhibit the formation of the tPa-PAI-1 complex with submicromolar IC(50). This class of compounds potentially represents a new generation of antithrombotic-fibrinolytic agents.
MeSH terms
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Blood Coagulation / drug effects
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Blood Coagulation Tests
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Fibrinolytic Agents / chemical synthesis*
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Fibrinolytic Agents / pharmacology
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Humans
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Inhibitory Concentration 50
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Plasminogen Activator Inhibitor 1 / metabolism*
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Protein Binding / drug effects
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Structure-Activity Relationship
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Thiophenes / chemical synthesis
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Thiophenes / pharmacology*
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Tissue Plasminogen Activator / antagonists & inhibitors*
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Tissue Plasminogen Activator / metabolism
Substances
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Fibrinolytic Agents
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Plasminogen Activator Inhibitor 1
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Thiophenes
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benzothiophene
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Tissue Plasminogen Activator