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目的:研究不同取代氨基侧链的引入对哒嗪酮类化合物抗血小板聚集活性的影响。方法:以乙酰基为连接片段,引入不同的取代氨基,设计合成一系列化合物;体外药理实验参考Born方法进行。结果:设计合成了10个目标化合物,其中8个未见报道,所有化合物均经过1HNMR等确证;所有化合物都具有抗血小板聚集的活性,其中化合物(6f)、(6g)、(6h)和(6j)的抗血小板聚集活性较强,化合物(6g)和(6j)的活性是6-[4-(吡啶基-4-氨基)苯基]-4,5-二氢-3(2H)哒嗪酮(MCI-154)的5倍。结论:引入不同的取代氨基对哒嗪酮类化合物抗血小板聚集的活性有影响。
Objective: To investigate the effect of different substituted amino side chains on the antiplatelet aggregation activity of pyridazinones. Methods: A series of compounds were designed and synthesized by introducing acetyl groups as the linker and different substituted amino groups. In vitro pharmacological experiments were performed according to Born method. RESULTS: Ten target compounds were designed and synthesized. Eight of them were not reported and all compounds were confirmed by 1H NMR. All of the compounds showed anti-platelet aggregation activity. Compounds (6f), (6g), (6h) and 6j) exhibited strong anti-platelet aggregation activity and the activity of compounds (6g) and (6j) was 6- [4- (pyridinyl-4- amino) phenyl] 5 times the imidazinone (MCI-154). Conclusion: The introduction of different substituted amino groups has an effect on the antiplatelet activity of pyridazinones.