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(E)-1,2-二芳基取代乙烯类化合物的合成及抗血小板聚集活性

Synthesis and anti-platelet aggregation activity of substituted (E)-1,2-diarylethene compounds

  • 摘要: 在2-溴苄基膦酸二乙酯结构基础上,合成两个系列(E)-1,2-二芳基取代乙烯类化合物 1~Ⅴ9 , 1~Ⅵ4 ),并对所合成的化合物进行抗血小板聚集活性实验。合成了13个未见文献报道的目标化合物,结构经元素分析、红外光谱、核磁共振氢谱、质谱确证。初步生物活性测试表明,多数化合物具有不同程度的抗血小板聚集活性,其中化合物 4、Ⅴ9 的活性较好。结果表明,(E)-1,2-二芳基取代乙烯类化合物是一类新型的具有潜在价值的抗血小板聚集活性的化合物。

     

    Abstract: Based on the analysis of the structure of diethyl 2-bromobenzylphosphonate,a series of substituted (E)-1,2-diarylethene compounds V1-V9 VI1-VI4 ) were synthesized,and their anti-platelet aggregation activities were evaluated.Their structures were confirmed by 1H NMR,IR and MS.It was found that most of the synthesized compounds possessed the anti-platelet aggregation activities,of which compounds V4 and V9 showed the most potent activities.Substituted(E)-1,2-diarylethene compounds are potentially new candidates as anti-platelet aggregation agents.〖