Design, synthesis and in vitro evaluation of potent, novel, small molecule inhibitors of plasminogen activator inhibitor-1

Bioorg Med Chem Lett. 2002 Apr 8;12(7):1063-6. doi: 10.1016/s0960-894x(02)00078-1.

Abstract

We have synthesized and evaluated a series of tetramic acid-based and hydroxyquinolinone-based inhibitors of plasminogen activator inhibitor-1 (PAI-1). These studies resulted in the identification of several compounds which showed excellent potency against PAI-1. The design, synthesis and SAR of these compounds are described.

Publication types

  • Comparative Study

MeSH terms

  • Chromogenic Compounds / chemistry
  • Drug Design
  • Drug Evaluation
  • Hydroxyquinolines / chemical synthesis*
  • Hydroxyquinolines / chemistry
  • Hydroxyquinolines / pharmacology*
  • In Vitro Techniques
  • Molecular Structure
  • Plasminogen Activator Inhibitor 1 / chemical synthesis*
  • Plasminogen Activator Inhibitor 1 / chemistry
  • Plasminogen Activator Inhibitor 1 / pharmacology*
  • Pyrrolidinones / chemistry*
  • Structure-Activity Relationship

Substances

  • Chromogenic Compounds
  • Hydroxyquinolines
  • Plasminogen Activator Inhibitor 1
  • Pyrrolidinones
  • tetramic acid