Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties

Bioorg Med Chem Lett. 2005 Jan 3;15(1):93-8. doi: 10.1016/j.bmcl.2004.10.026.

Abstract

A series of non-amide-linked 6-substituted-2-naphthamidine urokinase plasminogen activator (uPA) inhibitors are described. These compounds possess excellent binding activities and selectivities with significantly improved pharmacokinetic profiles versus previously described amide-linked inhibitors.

MeSH terms

  • Models, Molecular
  • Naphthalenes / chemistry
  • Naphthalenes / pharmacokinetics*
  • Plasminogen Inactivators / chemistry
  • Plasminogen Inactivators / pharmacokinetics*
  • Substrate Specificity
  • Urokinase-Type Plasminogen Activator / antagonists & inhibitors*

Substances

  • Naphthalenes
  • Plasminogen Inactivators
  • beta-naphthamidine
  • Urokinase-Type Plasminogen Activator