New fibrinolytic agents: benzothiophene derivatives as inhibitors of the t-PA-PAI-1 complex formation

Bioorg Med Chem Lett. 2003 May 19;13(10):1705-8. doi: 10.1016/s0960-894x(03)00233-6.

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

  • Blood Coagulation / drug effects
  • Blood Coagulation Tests
  • Fibrinolytic Agents / chemical synthesis*
  • Fibrinolytic Agents / pharmacology
  • Humans
  • Inhibitory Concentration 50
  • Plasminogen Activator Inhibitor 1 / metabolism*
  • Protein Binding / drug effects
  • Structure-Activity Relationship
  • Thiophenes / chemical synthesis
  • Thiophenes / pharmacology*
  • Tissue Plasminogen Activator / antagonists & inhibitors*
  • Tissue Plasminogen Activator / metabolism

Substances

  • Fibrinolytic Agents
  • Plasminogen Activator Inhibitor 1
  • Thiophenes
  • benzothiophene
  • Tissue Plasminogen Activator