5-羟甲基-2-呋喃甲醛衍生物的合成及降血糖活性评价

目的设计合成5-羟甲基-2-呋喃甲醛（5-HMF）衍生物，并评价其降血糖活性，寻找新型降血糖化合物。方法以5-羟甲基-2-呋喃甲醛为起始原料，分别经缩合、酯化、苄基化、脱苄基等反应合成目标化合物。通过测试目标化合物对葡萄糖促吸收率的影响评价化合物的活性。结果合成了14个未见文献报道的新化合物，其化学结构经。H—NIVlR、MS谱确证。结论生物活性评价结果显示，8个目标化合物（1～7、14）具有良好的降血糖活性，其中，化合物6的降血糖活性最好，其葡萄糖促吸收率为87．45％。

Synthesis and hypoglycemic activity of 5-hydroxylmethyl-2-furfural derivatives

5-Hydroxylmethyl-2-furfural(5-HMF) is the active ingredient of traditional Chinese medicine Trichosanthes kirilowii,which could lower the level of glycemic,so it is effective agents for the treatment of diabetes in clinic.However,it was reported that 5-HMF may have a weak cytotoxic,mutagenic,carcinogenic and other toxic side.The aim of this study is to discover new hypoglycemic drugs with high activities.Based on the structure of 5-HMF,fourteen new compounds were synthesized via condensation,esterification,protection and deprotection,whose structures were confirmed by 1H-NMR and MS.Eight compounds(1-7,14) were detected in vitro for hypoglycemic activity by observing their effects on absorption rate of glucose,all of them showed certain activities at 10 μg · mL-1 concentration,among which compound 6 exhibited the strongest hypoglycemic activity to insulin with 87.45% absorption rate of glucose.The activity was much better than the parent compound 5-HMF.The structure-activity relationship of its derivatives as a novel of hypoglycemic drugs will be investigated further.