作　　者： (黄志强）; (王媞媞）; (刘秀杰）;

机构地区： 天津理工大学化学化工学院,天津300384

出　　处： 《中国药物化学杂志》 2017年第4期274-278,共5页

摘　　要： 目的为寻找新的更高活性的抗血小板聚集药物,设计制得10个具有4-甲氧基-1,3-苯二磺酸酯结构的目标化合物(系列2);并对其进行体外活性筛选,评价其抗血小板聚集活性并推测其构效关系。方法按照前期工作获得的吡考他胺衍生物构效关系原则,进行了目标物设计合成,其结构均经~1H-NMR、IR和MS谱确证。采用Born比浊法对目标化合物进行了体外抗血小板聚集活性初筛。结果与结论合成的目标化合物均未见文献报道,其中PS27的活性最高,超过两个阳性对照药物吡考他胺和阿司匹林;PS22、PS23、PS24和PS26等4个化合物的活性优于或与对照药物相当。与磺酰胺类化合物相比,磺酸酯类中具有活性的化合物比例更高,在抗血小板聚集方面具有研究价值。 In this paper,we designed and synthesized ten target compounds on the basis of the structure of 4-methoxy-1,3-benzenedisulfonic acid ester（ series 2）. All the compounds are first reported in literature. Their antiplatelet aggregation effects were tested and assessed in vitro,and we can infer the structure-activity relationships from them. According to the principle of structure-activity relationship of picotamide derivatives obtained in previous work,the target compounds were designed and synthesized. The chemical structures of the compounds were confirmed by ~1H-NMR,IR and M S spectra. In vitro anti-platelet aggregation activities were assessed by using Born test. In the target compounds,PS27 had the highest activity and exceeded that of the two reference drugs picotamide and aspirin; In addition,PS22,PS23,PS24 and PS26 were superior to or equal to two control drugs. Comparing with sulfonamide compounds,the results showthat the percentage of the sulfonic esters compounds is higher and they are valuable in antiplatelet aggregation.

关 键 词： 抗血小板聚集 合成 甲氧基 苯二磺酸酯 吡考他胺