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.
|Number of pages||1|
|State||Published - Mar 1 2000|
- Antiaggregation activity
- Non-peptide fibrinogen receptor antagonists
- O-(4-aminoiminomethylphenyloxy)alkyl-N-substituted-L-tyrosine methyl esters