Synthesis and Biological Evaluation of Hydroxylcoumarin Derivatives as Antioxidant Agents  

作　　者：CHEN Chen WANG Ping ZOU Liwei YANG Ling FAN Yiming HU Wenzhong GE Guangbo 

机构地区：[1]College of Life Science, Dalian Minzu University, Dalian 116600, P. R. China [2]Laboratory of PharmaceuticaI Resource Discovery, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, R R. China

出　　处：《Chemical Research in Chinese Universities》2017年第2期194-199,共6页高等学校化学研究（英文版）

摘　　要：In this study, esculetin（1） was chosen as a lead compound and some structural modifications weredesigned to explore the antioxidant activities of esculetin derivatives. Meanwhile, a convenient method for selectivemethylation of catechol cournarins with different bases was developed. Furthermore, a few 5,7-dihydroxylcoumarinswere synthesized and 7-hydroxylcoumarins were employed in order to explore the potential structure-antioxidantactivity relationships. The antioxidant activities of these compounds were evaluated and compared with standardantioxidant Trolox by the 22＇-diphenyl-l-picrylhydrazyl（DPPH） assay, 2,2＇-azinobis-（3-ethylbenzthiazoline-6-sulfonate）cation（ABTS＋） assay and ferric reducing antioxidant power（FRAP） assay. The results show that the catechol group isthe key pharmacophore. Meanwhile, introducing electronegative groups at the C4 position of esculetin（1） mayenhance the antioxidative capacity, while introducing a group containing nitrogen as a hydrogen bond acceptor at theC8 position may slightly reduce the antioxidative capacity, Among them, the most powerful antioxidants are com-pounds 5 and 7, which exhibit higher antioxidant activity than esculetin（1） in all assays.

关 键 词：Hydroxylcoumarm ANTIOXIDANT activity RADICAL SCAVENGING effect STRUCTURE-ACTIVITY RELATIONSHIP 

分 类 号：O[理学]