4-甲氧基-1,3-苯二磺酸酯类化合物的合成及其体外抗血小
板聚集活性
黄志强;王媞媞;刘秀杰
【期刊名称】《中国药物化学杂志》 【年(卷),期】2017(027)004
【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1 H-NMR、IR和MS谱确证.采用Bom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 MS
4-甲氧基-1,3-苯二磺酸酯类化合物的合成及其体外抗血小板聚集活性
