1,3-二苯基-3-(苯胺基)-1-丙酮衍生物对α-葡萄糖苷酶抑制活性的研究  

Study on α-Glucosidase Inhibitory Activity of 1,3-Diphenyl-3-(phenylamino) propan-1-one Derivatives

作　　者：邱启东[1] 吴昊[1] 陈婵娟[1] 孙雯雯[1] 马林[1] 闫素君[1] 

机构地区：[1]中山大学化学与化学工程学院,广东广州510275

出　　处：《广东化工》2012年第6期1-3,22,共4页Guangdong Chemical Industry

摘　　要：利用Mannich反应合成了24个1,3-二苯基-3-(苯胺基)-1-丙酮衍生物(其中8个为新化合物),通过测定该系列化合物对α-葡萄糖苷酶活性半抑制浓度来评定其抑制活性,探索化合物分子中苯环上取代基对α-葡萄糖苷酶催化活性的影响。结果表明:新化合物24对α-葡萄糖苷酶的抑制活性稍好,IC50值为57.9μmol.L-1,其余大部分化合物对α-葡萄糖苷酶的IC50值大于100μmol.L-1,说明新化合物24苯环上取代基种类、数目和位置对α-葡萄糖苷酶抑制活性有明显的影响。动力学分析表明该系列化合物为α-葡萄糖苷酶的非竞争性抑制剂。Twenty-four compounds of 1,3-diphenyl-3-（phenylamino）-1-one derivatives,including eight new compounds,were synthesized via mannich reaction and their α-glucosidase inhibitory activities were evaluated.The results demonstrated that new compound 24 showed slightly better α-glucosidase inhibitory activity with the IC50 value 57.9 μmol·L-1,but most of the remaining compounds with IC50 value exceeded 100 μmol·L-1,which indicating that compound 24 had an absolutely effect on the α-glucosedase activity due to the specific substitutional groups on the aromatic rings.In addition,these compounds were found to be non-competitive inhibitors according to the kinetic analysis.

关 键 词：β-氨基酮衍生物 α-葡萄糖苷酶抑制活性 MANNICH反应 

分 类 号：TQ925.5[轻工技术与工程—发酵工程]