Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 2: (3-Substituted-5-halo-2-pyridinyl)guanidines

Bioorg Med Chem Lett. 2002 Jan 21;12(2):185-7. doi: 10.1016/s0960-894x(01)00702-8.

Abstract

Based on previous modeling predictions, a series of (3-substituted-5-chloro-2-pyridinyl)guanidines have been designed with good potency and selectivity for urokinase-type plasminogen activator (uPA). Compound 36 has a K(i) of 0.17 microM and greater than 300-fold selectivity with respect to tPA and plasmin.

MeSH terms

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

Substances

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