Synthesis and biological activity of non-peptide fibrinogen receptor antagonists(I)-N-substituted-O-(4-aminoiminomethylphenylamino) carbonylmethyl-L-tyrosine methyl ester

Tianlin Xu, Weiyi Hua, Peizhou Ni, Xuntian Jiang, Mengyu Bi, Yongmei Pei, Bing Yan

Research output: Contribution to journalArticlepeer-review

Abstract

AIM: To design and synthesize a class of compounds with inhibitory action upon ADP-induced platelet aggregation according to both the Arg-Gly-Asp(RGD) sequence and the non-peptide fibrinogen receptor antagonists that have been reported. METHODS: Tyrosine and 4-nitrobenzoic acid were used as the major reactants to obtain the target compounds by multi-step synthesis. Turbidometric technique was used to assess the inhibitory effects in vitro at 1 × 10-6 mol·L-1. RESULTS: Eighteen compounds of N-substituted-O-(4-aminoiminomethylphenylamino)carbonylmethyl-L-tyrosine methyl ester were synthesized, ten (Ia, f, g, i∼m, q, r) of them showed inhibitory action at the above concentrations while Ig with inhitory rate of 64% is the most potent one. CONCLUSION: All of the eighteen compounds are new compounds, and most of them showed antiaggregation action on platelet rich-plasma.

Original languageEnglish
Pages (from-to)432-433
Number of pages2
JournalYaoxue Xuebao
Volume34
Issue number6
StatePublished - Jun 1 1999

Keywords

  • Antiaggregation action
  • Design
  • N-substituted-O-(4-aminoiminomethylphenylamino)carbonylmethyl-L-tyrosine methyl ester
  • Non-peptide fibrinogen receptor antagonists
  • Synthesis

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