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目的：６（４′取代苯基）４，５二氢３（２Ｈ）哒嗪酮类化合物的合成及抗血小板聚集活性的研究。方法：通过付克反应、碳链延长、水解和环合反应得到两个关键中间体，然后通过酰化反应制得各种酰胺化合物；参考Ｂｏｒｎ比浊法测定目标化合物的抗血小板聚集活性。结果：设计合成了２４个６（４′取代酰胺基苯基）４，５二氢３（２Ｈ）哒嗪酮类化合物，２２个为首次报道；所有化合物在体外对ＡＤＰ诱导的兔血小板聚集均有不同程度的抑制作用，第ＩＩ类化合物的抑制作用强于第Ｉ类化合物，其中Ｉ１，Ｉ３，ＩＩ１，Ｉ３，ＩＩ４，Ｉ６和ＩＩ９的抑制作用均强于对照药ＣＩ９３０，其中Ｉ１和ＩＩ３的抑制作用最强，其ＩＣ５０约为ＣＩ９３０的１／１０。结论：其中一些化合物显示较强的抗血小板聚集活性，值得进一步研究。
Objective: To study the synthesis and anti-platelet aggregation activity of 6 (4’-substituted phenyl) 4,5dihydro3 (2H) pyridazinones. Methods: Two key intermediates were obtained by Friedel-Crafts reaction, extension of carbon chain, hydrolysis and cyclization reaction, and then various amide compounds were obtained by acylation reaction. The anti-platelet aggregation activity of the target compounds was measured by Born turbidimetry. RESULTS: Twenty-four (6’-substituted amidophenyl) -4,5-dihydro-3 (2H) pyridazinones were designed and synthesized, of which 22 were reported for the first time. Induced rabbit platelet aggregation had different degree of inhibition, the inhibitory effect of class II compounds is stronger than the class I compounds, of which I1, I3, II1, I3, II4, I6 and II9 inhibition were stronger than the control drug CI 930, of which I1 and II3 the strongest inhibitory effect, the IC50 about CI 1/930. Conclusions: Some of these compounds show strong anti-platelet aggregation activity and deserve further study.