Isoxazoline GPIIb/IIIa antagonists bearing a phosphoramidate

Bioorg Med Chem Lett. 1999 Jan 18;9(2):123-6. doi: 10.1016/s0960-894x(98)00709-4.

Abstract

Isoxazolinylacetamides bearing a phosphoramidate group alpha- to the carboxylate moiety (3) were prepared and evaluated for in vitro antiplatelet efficacy. They were found to bind GPIIb/IIIa with high affinity and were potent antagonists of ADP mediated platelet aggregation.

MeSH terms

  • Animals
  • Blood Platelets / chemistry
  • Calcium / pharmacology
  • Citric Acid / pharmacology
  • Dogs
  • Drug Design
  • Heparin / pharmacology
  • Humans
  • Inhibitory Concentration 50
  • Isoxazoles / administration & dosage
  • Isoxazoles / pharmacology*
  • Platelet Aggregation Inhibitors / pharmacology
  • Platelet Glycoprotein GPIIb-IIIa Complex / antagonists & inhibitors*
  • Platelet Glycoprotein GPIIb-IIIa Complex / chemistry*

Substances

  • Isoxazoles
  • Platelet Aggregation Inhibitors
  • Platelet Glycoprotein GPIIb-IIIa Complex
  • Citric Acid
  • Heparin
  • Calcium