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目的寻找活性更好的抗血小板聚集化合物。方法基于吡考他胺的抗血小板聚集机制和生物电子等排原理,以2,3-二甲基苯酚为原料,经Williamson反应、氧化、氯代和胺解反应合成了13个未见文献报道的4-乙氧基-N,N’-二(取代苯基)酰胺类化合物。以吡考他胺和阿司匹林为阳性对照药物,采用Born比浊法对目标化合物进行活性筛选。结果与结论目标化合物的结构经MS、IR和1H-NMR谱确证,其中,4个目标化合物(7、9、10和12)的抗血小板聚集活性明显高于阳性对照药吡考他胺,有进一步研究的价值。在活性筛选结果的基础上对目标化合物的构效关系作了初步的推测和总结,以期为今后开展相关研究提供借鉴。
Objective To find a more active anti-platelet aggregation compound. Methods Based on the anti-platelet aggregation mechanism and bioisosterism of picotamide, 2,3-dimethylphenol was used as a starting material to synthesize 13 unreported reports by Williamson reaction, oxidation, chlorination and aminolysis Of 4-ethoxy-N, N’-bis (substituted phenyl) amides. Pyrimetamide and aspirin were used as positive control drugs, and the target compounds were screened by Born turbidimetry. RESULTS AND CONCLUSIONS The structures of the target compounds were confirmed by MS, IR and 1H-NMR spectra. Among them, the anti-platelet aggregation activities of four target compounds (7, 9, 10 and 12) were significantly higher than that of the positive control drug The value of further research. The structure-activity relationship of the target compounds was preliminarily estimated and summarized on the basis of the activity screening results in order to provide reference for the future research.