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, 合成, 脂质过氧化

Abstract: 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 IC₅₀ were 30,22.7,17.7,22.2 and 24μmol·L^-1,respectively.

Key words: Ebselen, Benzisoselenazolone, Amino acid derivatives, Synthesis, Lipid peroxidation