摘要
目的探讨取代苯基羧酸衍生物的合成及抑制血小板聚集作用。方法以苯甲醚为起始原料 ,设计并合成了 11个未见文献报道的目标化合物 ,这些化合物均为取代苯基羧酸衍生物 ,其中 7个化合物具有磺酰胺结构 ,4个具有酰胺结构。结果目标化合物的结构经IR、1H NMR和MS光谱确证。采用Born比浊法对目标化合物抑制血小板聚集作用进行了初步筛选测定。结论多数目标化合物都有不同程度的抑制ADP诱导血小板聚集作用 ,化合物 4f活性最强 ,优于已上市药物picotamide。
Aim To explore the potential inhibition of platelet aggregation and synthesis of substituted benzene carboxylic acid derivatives.Method Eleven of arylsulfonamide and arylamide derivatives have been prepared from anisole in good yields.Result The structures of those compounds were confirmed by IR,~1H-NMR and MS analysis.Their activities against platelet aggregation were tested in vitro by using the Born test in rabbits.Conclusion The results showed the compound 4f had potent antiplatelet aggregation activity as the drugs of picotamide.
出处
《中国药物化学杂志》
CAS
CSCD
2004年第3期140-143,共4页
Chinese Journal of Medicinal Chemistry
