CAJ | 학술논문

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。
이용Mannich반응합성료24개1,3-이분기-3-（분알기）-1-병동연생물（기중8개위신화합물）,통과측정해계렬화합물대α-포도당감매활성반억제농도래평정기억제활성,탐색화합물분자중분배상취대기대α-포도당감매최화활성적영향。결과표명：신화합물24대α-포도당감매적억제활성초호,IC50치위57.9μmol.L-1,기여대부분화합물대α-포도당감매적IC50치대우100μmol.L-1,설명신화합물24분배상취대기충류、수목화위치대α-포도당감매억제활성유명현적영향。동역학분석표명해계렬화합물위α-포도당감매적비경쟁성억제제。
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.