含多氟的4-甲基噻唑环的新型二肽基肽酶Ⅳ抑制剂的合成及其降血糖活性  

Synthesis and anti-Hyperglycemic Activities of Bearing Multi Fluorine 4-Methylthiazole Compounds as Novel Dipeptidyl Peptidase Ⅳ Inhibitors

作　　者：罗杰[1] 赵桂龙[2] 王玉丽[3] 邵华[3] 曲宝涵[1] 汤立达[4] 

机构地区：[1]青岛农业大学化学与药学院,山东青岛266109 [2]天津药物研究院,天津300193 [3]天津药物研究院天津市分子设计与药物发现重点实验室,天津300193 [4]天津药物研究院药代动力学与药效学省部共建国家重点实验室,天津300193

出　　处：《合成化学》2011年第1期41-44,61,共5页Chinese Journal of Synthetic Chemistry

基　　金：科技部支撑计划资助项目(2007BAI40B01)

摘　　要：设计并合成了一系列含多氟的4-甲基噻唑环的新型二肽基肽酶Ⅳ抑制剂(6a～6i),其结构经1H NMR和ESI-MS表征。以西他列汀为阳性对照药,采用小鼠体内口服葡萄糖耐受量法测试,结果显示6c和6h具有明显的降血糖作用。A series of novel dipeptidyl peptidase Ⅳ inhibitors（6a～6j） bearing multi fluorine atoms were designed and synthesized.The structures were characterized by 1H NMR and ESI-MS.Their anti-hyperglycemic activities were evaluated through in vivo oral glucose tolerance test in mice.The results showed that 6c and 6h were found to be comparable with the positive control sitagliptin.

关 键 词：多氟 4-甲基噻唑 二肽基肽酶Ⅳ 合成 降血糖活性 

分 类 号：O626[理学—有机化学] R914.5[理学—化学]