摘要
本文设计合成了一系列曲酸三氮唑类化合物,并考察了所合成化合物的抑制酪氨酸酶活性、抑制α-葡萄糖苷酶活性及抗氧化活性。结果表明,大部分化合物具有良好的抑制酪氨酸酶活性和抑制α-葡萄糖苷酶活性,其中化合物5f的抑制酪氨酸酶活性最好,其IC50值为3.28μmol·L^(-1),约为曲酸的8倍,化合物5i对α-葡萄糖苷酶抑制活性最好,IC50值为14.42μmol·L^(-1)。所有化合物都具有一定的抗氧化活性。抑制机理研究表明:化合物5f为可逆混合型酪氨酸酶抑制剂,化合物5i为不可逆α-葡萄糖苷酶抑制剂。
A series of triazoles of kojic acid were synthesized,and their inhibitory tyrosinase activity,α-glucosidase activity and antioxidant activity were investigated.The results showed that most of the compounds had potent tyrosinase inhibitory activities andα-glucosidase inhibitory activities.Compound 5f had the most potent inhibition of tyrosinase activity with IC50 value of 3.28μmol·L^(-1),which was about 8 times that of kojic acid.Compound 5i had the most potentα-glucosidase inhibitory activity.The IC50 value was 14.42μmol·L^(-1).All compounds showed certain antioxidant activity.The inhibition mechanism showed that compound 5f was a reversible mixed tyrosinase inhibitor and compound 5i was an irreversibleα-glucosidase inhibitor.
作者
刘丹
彭子祥
刘进兵
LIU Dan;PENG Zi-xiang;LIU Jin-bing(School of Food and Chemical Engineering,Shaoyang University,Shaoyang 422099,China)
出处
《化学研究与应用》
CAS
北大核心
2023年第2期311-317,共7页
Chemical Research and Application
基金
湖南省教育厅项目(19C1632)资助
湖南省自然科学基金项目(2022JJ50189)资助
邵阳学院研究生科研创新项目(CX2021SY063)资助。
关键词
曲酸三氮唑类化合物
生物活性
抑制机理
合成
triazole kojic acid compounds
biological activity
inhibition mechanism
synthesis
