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为寻找效果更好的降血糖药物以及进一步研究列奈类化合物的构效关系,以米格列奈为先导物,设计、合成具有降血糖活性的α-苄基取代的琥珀酸单酰胺类化合物。以丁二酸二乙酯和各种取代苯甲醛为原料,经缩合、水解得苯亚甲基丁二酸,再进行酸酐化、胺解和氢化等反应合成了12个目标化合物,化合物结构通过元素分析、IR、1HNMR和ESI-MS得以确证,并测定了它们的降血糖活性。初步药理试验表明所合成的化合物中6c、6e和6g降糖作用较明显,其中6e较为突出,其降糖作用与那格列奈相当。
In order to find better hypoglycaemic drugs and to further study the structure-activity relationship of lenecline compounds, mitiglinide was used as a leader to design and synthesize α-benzyl substituted succinic monoamide compounds with hypoglycemic activity . Using diethyl succinate and various substituted benzaldehydes as raw materials, 12 target compounds were synthesized by condensation and hydrolysis of succinic acid with succinic acid, then with amine, hydrogenation and the like. The structures of the compounds were confirmed by Elemental analysis, IR, 1H NMR and ESI-MS were confirmed and their hypoglycemic activity was determined. Preliminary pharmacological tests showed that the compound 6c, 6e and 6g hypoglycemic effect more obvious, of which 6e more prominent, its hypoglycemic effect and nateglinide equivalent.