Design and synthesis of oxadiazolidinediones as inhibitors of plasminogen activator inhibitor-1

Bioorg Med Chem Lett. 2004 Jul 5;14(13):3477-80. doi: 10.1016/j.bmcl.2004.04.058.

Abstract

A novel series of PAI-1 inhibitors containing an oxadiazolidinedione moiety were identified by high through-put screening. Optimization of substituents by parallel synthesis and the iterative design toward understanding structure-activity relationship to improve potency are described.

MeSH terms

  • Drug Design
  • Humans
  • Inhibitory Concentration 50
  • Isomerism
  • Microscopy, Fluorescence
  • Oxazolidinones / chemical synthesis
  • Oxazolidinones / pharmacology
  • Plasminogen Activator Inhibitor 1 / metabolism*
  • Structure-Activity Relationship

Substances

  • Oxazolidinones
  • Plasminogen Activator Inhibitor 1