Novel synthetic RGD analogs incorporating salicylic acid derivatives show antiplatelet activity in vitro

Yiannis M. Sarigiannis, George P. Stavropoulos, Maria T. Liakopoulou-Kyriakides, Pantelis E. Makris

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

Continuing our investigational efforts for more active GpIIb/IIIa inhibitors we have synthesized four novel RGD (Arg-Gly-Asp) analogs incorporating salicylic acid derivatives at their N-terminal amino group using the solid phase synthesis. The synthesized compounds 5-Cl-2-HO-C6H3-CO-Arg-Gly-Asp(OBzl)-NH2 and 5-Br-2-HO-C6H3-CO-Arg-Gly-Asp(OBzl)-NH2 were tested for their inhibitory activity on human platelet aggregation in vitro and found to be potent inhibitors of the platelet aggregation with 75 and 67% inhibitory activity respectively. In order to confirm our results flow cytometry with monoclonal antibodies against GpIb, GpIIb/IIIa, GpIIIa and GMP140 receptors was used.

Original languageEnglish
Pages (from-to)101-109
Number of pages9
JournalLetters in Peptide Science
Volume9
Issue number2-3
DOIs
Publication statusPublished - 2002

Keywords

  • GpIIb/IIIa inhibitors
  • Inhibitory activity
  • Platelet aggregation
  • RGD analogs
  • Salicylic acid derivatives

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