【摘要】 目的:研究米格列奈类似物的合成及其降血糖作用。方法:由丁二酸二甲酯经缩合、水解、酸酐化、胺解、氢化和成盐等反应合成目标物;测定目标物的降血糖效果。结果:合成了13个新的中间体和13个新目标化合物,其结构经IR,1H NMR和ESI-MS质谱确证。结论:初步降血糖活性测试表明,目标化合物XL 03、XL06、XL 08和XLH 01对正常小鼠有明显的降血糖活性,其中化合物XL 06降低血糖的作用与米格列奈相当。更多还原

【Abstract】 AIM:To study the synthesis and hypoglycemic activity of mitiglinide analogues.METHODS:The target compounds were synthesized from dimethyl succinate via condensation,hydrolysis,anhydridization,amidation,hydrogenization and salification reactions.The hypoglycemic activities of target compounds were evaluated.RESULTS:Thirteen new intermediates and thirteen new target compounds,which were never reported,were synthesized.Structures of all the compounds were confirmed by IR,（）¹H NMR and ESI-MS.CONCLUSION:The pharmacological study showed that four new mitiglinide analogues（XL 03,XL 06,XL 08 and XLH 01） exhibited considerable hypoglycemic activity.XL 06 showed the same hypoglycemic potency as mitiglinide.更多还原