Synthesis and antiaggregation activity of O-(4-aminoiminomethylphenyloxy) alkyl-N-substituted-L-tyrosine methyl esters

Tianlin Xu, Xuntian Jiang, Peizhou Ni, Weiyi Hua, Yongmei Pei

Research output: Contribution to journalArticle

Abstract

AIM: The synthesis and antiaggregation activity of a series of compounds with p-amidinophenyl group and tyrosine methyl esters as their terminals were studied. METHODS and RESULTS: A series of O-(4-aminoiminomethylphenyloxy)alkyl-N-substituted-L-tyrosine methyl esters were prepared from 4-cyanophenol, L-tyrosine and different dihalo-alkanes. All compounds (IVa∼i) were new compounds. Their in vitro activity against ADP-induced platelet aggregation were tested. The structure-activity relationships were discussed. CONCLUSION: Some of the compounds showed antiaggregation activity on platelet rich-plasma at the final concerntration of 1 × 10-6 mol·L-1. The potency of IVa ∼ i showed that compounds with three methylene groups are better than those with four methylene groups on the same R-substituent in the above series of compounds.

Original languageEnglish
Number of pages1
JournalYaoxue Xuebao
Volume35
Issue number3
StatePublished - Mar 1 2000
Externally publishedYes

Keywords

  • Antiaggregation activity
  • Non-peptide fibrinogen receptor antagonists
  • O-(4-aminoiminomethylphenyloxy)alkyl-N-substituted-L-tyrosine methyl esters

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