Ebselen氨基酸衍生物的合成及抗脂质过氧化作用  

The Synthesis and Anti-lipid Peroxidation Activity of Amino Acid Derivatives of Ebselen

作　　者：肖颖歆[1] 刘秀芳[1] 徐汉生[1] 孙士勇[1] 徐波[1] 

机构地区：[1]武汉大学化学系,北京医科大学天然药物及仿生药物国家重点实验室

出　　处：《高等学校化学学报》1996年第6期914-916,共3页Chemical Journal of Chinese Universities

摘　　要：Ｅｂｓｅｌｅｎ氨基酸衍生物的合成及抗脂质过氧化作用肖颖歆，刘秀芳，徐汉生，孙士勇，徐波（武汉大学化学系，武汉，４３００７２）（北京医科大学天然药物及仿生药物国家重点实验室）关键词２－苯基－１，２－苯并异硒唑－３（２Ｈ）－酮，苯并异硒唑酮，氨基酸衍生物...Amino acid was used as a carrier of the active molecule──ebselen,which mimicked the properties of GSH-Px and was known as an anti-inflammatory drug.Eiht ebselen derivatives with amino acdethyl esters attached to the p-position of 2-phenyl moiety were prepared.2-(4'- Carboxylphenyl)-1,2-benzisoselenazol-3(2H)-one(1) was used as the intermediate prepared in good yield by cyclization of 2-chloroselenobenzoyl chloride with 4-amino benzoic acid in the presence of Et3N. Then l was treated with p-toluenesulfonates of amino acid ethyl ester,and the target compounds were obtained by further purification,Effects of compounds 1,2,3,4 as well as ebselen on Fe￣(2+)/cysteine-induced rat liver microsomal peroxidation were studied.Their IC_(50) were 30,22. 7,17.7,22.2 and 24μmol￣(-1),respectively.

关 键 词：脂质过氧化 苯并异硒唑酮 有机硒化合物 

分 类 号：O627.61[理学—有机化学]