Synthesis and antiaggregatory activity of RGD-peptidomimetics based on 4-oxo-4-(piperazine-1-yl)butyric acid as Arg-mimetic

Acta Pol Pharm. 2003 Sep-Oct;60(5):375-81.

Abstract

A scheme of synthesis of previously obtained RGDF-peptidomimetic-4-oxo-4-(piperazine-1-yl)butyrylglycyl-D,L-beta-phenyl-beta-alanine (I), was simplified. The novel RGDF-peptidomimetic -4-oxo-4-piperazine-1-yl)butyryl-glycyl-L-aspartyl-L-phenylalanine (II) was synthesized with the use of 4-oxo-4-(piperazine-1-yl)butyric acid as arginyl mimetic. The obtained pseudopeptides were able to inhibit both platelet aggregation in human blood and binding of fibrinogen to its receptor.

MeSH terms

  • Blood Platelets / metabolism
  • Chemistry, Pharmaceutical
  • Fibrinogen / metabolism
  • Humans
  • In Vitro Techniques
  • Molecular Mimicry
  • Oligopeptides / chemical synthesis*
  • Oligopeptides / chemistry*
  • Oligopeptides / pharmacology
  • Piperazines / chemical synthesis*
  • Piperazines / chemistry
  • Piperazines / pharmacology
  • Platelet Aggregation Inhibitors / chemical synthesis*
  • Platelet Aggregation Inhibitors / chemistry
  • Platelet Aggregation Inhibitors / pharmacology
  • Protein Binding

Substances

  • 4-oxo-4-(piperazine-1-yl)butyryl-glycyl-L-aspartyl-L-phenylalanine
  • Oligopeptides
  • Piperazines
  • Platelet Aggregation Inhibitors
  • arginyl-glycyl-aspartic acid
  • Fibrinogen