Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines

Bioorg Med Chem Lett. 2002 Jan 21;12(2):181-4. doi: 10.1016/s0960-894x(01)00701-6.

Abstract

The identification of 2-pyridinylguanidines (e.g., 27 and 28) as selective inhibitors of urokinase-type plasminogen activator (uPA) is described. The X-ray crystal structure of 27 has been determined, and modelling has been used to predict binding in the enzyme active site.

MeSH terms

  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Guanidines / chemistry
  • Guanidines / pharmacology*
  • Models, Molecular
  • Pyridines / chemistry*
  • Urokinase-Type Plasminogen Activator / antagonists & inhibitors*
  • X-Ray Diffraction

Substances

  • Enzyme Inhibitors
  • Guanidines
  • Pyridines
  • Urokinase-Type Plasminogen Activator
  • pyridine