4,5-二氢-3(2H)-哒嗪酮类化合物的合成及其对血小板聚集的抑制作用
Synthesis and the antiplatelet aggregative activity of 4,5-dihydro-3(2 H)-pyridazinones
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摘要: 目的: 合成新的哒嗪酮类化合物,并研究其抗血小板凝集活性。 方法: 在6-(4-氯乙酰氨基苯基)-4,5-二氢-3(2H)哒嗪酮引入不同取代哌嗪,合成一系列化合物,并经过1H-NMR等确证;参考Born方法进行体外药理实验。 结果: 所有化合物都具有抗血小板凝集的活性,其中化合物(1)、(4)的抗血小板凝集活性明显优于MCI-154。 结论: 4-位取代哌嗪环基的引入对化合物抗血小板凝集的活性有显著影响。Abstract: Objective: To study the antiplatelet aggregative activity of 6-(4-substituted acetamido-phenyl)-4,5-dihydro-3(2H)-pyridazinones inletting different piperazine groups. Methods: Ten target compounds were designed and synthesized.All of them were confirmed by 1H-NMR spectra.Born method was applied for preliminary pharmacological test in vitro. Results: All of the target compounds were reported.The results of preliminary pharmacological test showed that all the target compounds exhibited potent antiplatelet aggregative activity to a certain extent.Compound(1)/(4)and performed better than MCI-154 in vitro. Conclusion: The carbochain’s length of piperazine’s 4-substituted groups impacted the antiplatelet aggregative activity promintly.
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Key words:
- chemical synthesis /
- pyridazinones /
- antiplatelet aggregative activity /
- in vitro
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