Novel fibrinogen receptor antagonists. RGDF mimetics, derivatives of 4-(isoindoline-5-yl)amino-4-oxobutyric acid

Bioorg Med Chem Lett. 2004 Nov 15;14(22):5533-5. doi: 10.1016/j.bmcl.2004.09.002.

Abstract

The novel RGDF mimetics 9a and 9b were synthesized with the use of 4-(isoindoline-5-yl)amino-4-oxobutyric acid as a surrogate of Arg-Gly motif. The synthesized compounds have demonstrated a high potency to inhibit platelet aggregation in vitro and to block FITC-Fg binding to alpha(IIb)beta(3) on washed human platelets.

MeSH terms

  • Butyrates / chemical synthesis*
  • Butyrates / chemistry
  • Butyrates / pharmacology*
  • Drug Evaluation, Preclinical
  • Humans
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Indoles / pharmacology*
  • Isoindoles
  • Molecular Mimicry
  • Molecular Structure
  • Oligopeptides / chemical synthesis*
  • Oligopeptides / chemistry
  • Oligopeptides / pharmacology*
  • Platelet Aggregation / drug effects
  • Platelet Aggregation Inhibitors / chemical synthesis*
  • Platelet Aggregation Inhibitors / chemistry
  • Platelet Aggregation Inhibitors / pharmacology*
  • Platelet Membrane Glycoproteins / antagonists & inhibitors
  • Receptors, Fibrinogen / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • 4-(isoindoline-5-yl)amino-4-oxobutyric acid
  • Butyrates
  • Indoles
  • Isoindoles
  • Oligopeptides
  • Platelet Aggregation Inhibitors
  • Platelet Membrane Glycoproteins
  • Receptors, Fibrinogen
  • arginyl-glycyl-aspartyl-phenylalanine