摘要
以1,2-二甲氧基苯,丁二酸酐以及α-溴代四乙酰基吡喃糖为原料,设计并合成了作为SGLT2抑制剂的两个结构新颖的苯萘基糖苷化合物(6a和6b),其结构经1HNMR,13C NMR,IR和ESI-MS确认。利用小鼠体内葡萄糖耐受量法测定了6治疗糖尿病的活性,结果发现6a具有明显的降血糖作用,其活性与阳性对照药格列齐特相当。
Two novel phenylnaphthyl glycoside compounds （6a and 6b） were designed and synthesized as SGLT2 inhibitors from 1,2-dimethoxybenzene, succinic anhydride and tetra-O-acetyl-α-gly- copyranosyl bromides. The structures were characterized by 1H NMR, 13C NMR, IR and ESI-MS. Anti-diabetic activity was performed through in vivo by oral glucose tolerance test in mice. The preliminary pharmacological test of 6 showed that 6a was able to decrease blood glucose significantly using Gliclazide as a positive control drug.
出处
《合成化学》
CAS
CSCD
北大核心
2009年第5期570-573,共4页
Chinese Journal of Synthetic Chemistry
基金
科技部支撑计划资助项目(2007BAI40B01)
