3-氨基-7,8-二甲氧基香豆素及其衍生物的合成及抗氧化活性  

Synthesis and Antioxidation Activity of 3-Amino-7,8-dimethoxycoumarin and Its Derivatives

作　　者：陈琳 闵曼 林吉娣 CHEN Lin;MIN Man;LIN Jidi(College of Pharmacy,Guangdong Pharmaceutical University,Guangzhou 510006,China;Guangzhou Huibiao Testing Technology Center,Guangzhou 510670,China)

机构地区：[1]广东药科大学药学院,广州510006 [2]广州汇标检测技术中心,广州510670

出　　处：《应用化学》2020年第12期1420-1425,共6页Chinese Journal of Applied Chemistry

基　　金：广东省科技计划项目(2012B061700040);广东省医学科学技术研究基金项目(201618171249486)资助。

摘　　要：合成了3-氨基-7,8-二甲氧基香豆素及其衍生物共11个化合物,其中3个化合物(2b、2d、2e)为新型香豆素芳酰胺类化合物。通过猝灭1,1-二苯基-2-三硝基苯肼(DPPH)、2,2′-联氮二(3-乙基苯并噻唑-6-磺酸)二铵盐阳离子自由基(ABTS+·)和羟自由基实验考察了所合成化合物的抗氧化活性,结果表明化合物2b对DPPH自由基、羟自由基的清除能力超出或接近对照品维生素C,而衍生物2a、2b和2c的抗氧化活性优于母体。故酰化可提高3-氨基-7,8-二甲氧基香豆素的抗氧化性能,尤其是普遍提高了羟基自由基的清除能力。Eleven coumarin compounds with aromatic amide skeletons were synthesized.The antioxidant activities of the synthesized compounds were investigated by quenching 1,1-diphenyl-2-picrylhydrazyl radical(DPPH),2,2′-azinobis(3-ethylbenzothiazoline-6-sulphonate)ammonium salt cationic radical(ABTS+·)and hydroxyl radicals.The results show that the scavenging ability of compound 2b to DPPH radicals and hydroxyl radicals is beyond or close to that of the control vitamin C,while the antioxidant activity of derivatives 2a,2b and 2c is better than that of the parent.Therefore,acylation is a promising way to improve the antioxidant capacity of 3-amino-7,8-dimethoxycoumarin,especially the scavenging capacity of hydroxyl radicals.

关 键 词：3-氨基-7 8-二甲氧基香豆素类 合成 抗氧化 

分 类 号：O626[理学—有机化学]