SYNTHESIS AND BIOLOGICAL ACTIVITY OF NON-PEPTIDEFIBRINOGEN RECEPTOR ANTAGONISTS(I)-N-SUBSTITUTED-O-(4-AMINOIMINOMETHYLPHENYLAMINO) CARBONYL-METHYL-L-TYROSINE METHYL ESTER

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.