摘要
从6-羟基托品酮出发,经过羟基的乙酰基化和苯甲酰基化,再通过还原氨化高效地得到含有活泼胺基的2个母核化合物。2个母核化合物与不同的酰氯反应,得到一系列托品酮衍生物。该衍生物经过体外过氧化物酶增生因子活化受体γ亚型(PPARγ)激活、二肽基肽酶Ⅳ(DPP-Ⅳ)抑制实验,发现多数化合物对DPP-Ⅳ显示抑制活性,其中2个化合物(3μmol/L DMSO溶液)对DPP-Ⅳ抑制率超过30%。
6-Hydroxytropinone was chosen as the primary precursor and subjected to a series of reactions including aeetylation or benzoylation of its hydroxyl group, reduction and ammoniation of its keto group to yield two compounds containing tropane with primary amine core structure. A series of N-aeyl compounds has been prepared by the reactions of the core structures with a variety of acyl chlorides. These compounds were screened in peroxisome proliferateive aetiveated recaptor-γ （PPARγ） and dipeptidylpeptidase-Ⅳ （DPP-IV） invitro models. Most of these compounds displayed inhibitory effect against DPP-Ⅳ and two of them showed inhibitory rates higher than 30% at 3μmol/L in DMSO. But no activation toward PPARγ of all compounds could be observed.
出处
《应用化学》
CAS
CSCD
北大核心
2013年第10期1127-1132,共6页
Chinese Journal of Applied Chemistry
基金
湖南省科技计划重大专项
长沙市科技局重点项目(2010FJ1010
k1003212-31)
关键词
托品酮衍生物
糖尿病
体外
二肽基肽酶Ⅳ抑制活性
tropinone derivaties, diabetes, in-vitro model, dipeptidylpeptidase-Ⅳ inhibitory effect
