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目的：根据ＲＧＤ肽及目前活性较好的非肽类纤维蛋白原受体拮抗剂的结构特点，设计、合成一系列有抗血小板聚集活性的化合物。方法：以酪氨酸及对硝基苯甲酸等为主要原料经多步合成，对所得化合物用比浊法测定在１×１０－６ｍｏｌ·Ｌ－１时对体外血小板聚集的抑制率。结果：合成了１８个Ｎ取代Ｏ对甲脒苯胺基羰甲基Ｌ酪氨酸甲酯类化合物（Ｉａ～ｒ），均为新化合物。结论：其中１０个化合物（Ｉａ，ｆ，ｇ，ｉ～ｍ，ｑ，ｒ）显示一定的活性，活性最高的（Ｉｇ）抑制率达６４％。
OBJECTIVE: To design and synthesize a series of compounds with anti-platelet aggregation activity according to the structural characteristics of RGD peptide and the currently active non-peptide fibrinogen receptor antagonist. Methods: The tyrosine and p-nitrobenzoic acid as the main raw material were synthesized by multi-step method. The inhibitory rate of the obtained compound to platelet aggregation in vitro was determined by turbidimetry at 1 × 10-6 mol·L-1. RESULTS: Eighteen N-substituted O formamidine carbonyl methyl L tyrosine methyl ester compounds (Ia ~ r), are new compounds. Conclusion: Among them, 10 compounds (Ia, f, g, i ~ m, q, r) showed certain activity with the highest activity (Ig) inhibition rate of 64%.