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

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。

Abstract: AimTo design and synthesize new compounds of prandial glucose regulator with more simple structure. MethodsThe 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. ResultsSeventeen compounds had different hypoglycemic activeity in mice, among them, 9 compounds had higher hypoglycemic activity and 6 compounds had character of prandial glucose regulator. ConclusionPart of the compounds have higher hypoglycemic activity deserve to be further investigated.