苄叉基琥珀酸类衍生物的合成及降糖活性  

Synthesis and insulinotropic activity of 2-benzylidenesuccinic acid derivatives

作　　者：高丽梅[1] 杨鹏[1] 宋丹青[1] 

机构地区：[1]中国医学科学院中国协和医科大学医药生物技术研究所,北京100050

出　　处：《药学学报》2005年第12期1122-1126,共5页Acta Pharmaceutica Sinica

摘　　要：目的设计合成结构更为简单的餐时血糖调节剂。方法以丁二酸二乙酯与苯甲醛或对氟苯甲醛为起始原料,经缩合、水解、脱水得到酸酐,再分别与不同的芳香胺、脂肪胺及氮杂环进行酰胺化,共合成了18个衍生物。利用核磁共振谱、质谱和红外光谱进行结构确认。结果小鼠体内实验表明:剂量为3.0 mg.kg-1时,18个衍生物中17个表现出不同程度的降糖活性,其中9个具有较好的降糖活性,6个具有餐时血糖调节剂的特点。结论部分化合物具有较好的降糖活性,待进一步研究。Aim To design and synthesize new compounds of prandial glucose regulator with more simple structure. Methods The target compounds were synthesized from diethyl succinate and benzaldehyde or 4-fluorobenzaldehyde by four-step reactions. Thus 18 compounds were synthesized. Their structures were comfirmed by NMR, MS and IR. Results Seventeen compounds had different hypoglycemic activeity in mice, among them, 9 compounds had higher hypoglycemic activity and 6 compounds had character of prandial glucose regulator. Conclusion Part of the compounds have higher hypoglycemic activity deserve to be further investigated.

关 键 词：苄叉基琥珀酸类衍生物 合成 餐时血糖调节剂 

分 类 号：R916.4[医药卫生—药学]