苯并异硒唑酮氨基酸衍生物的合成及抗脂质过氧化作用

在已知具有氧化作用的2-苯基-1,2-苯并异硒唑-3(2H)-酮(Ebselen)的基础上, 将其2-位苯环更换成氨基酸乙酯, 设计并合成了9个苯并异硒酮的氨基酸衍生物3～11. 这类化合物的抗氧化作用药理研究表明,它们对Fe^2^+/半胱氨酸及维生素C诱发的大鼠肝微粒体脂质过氧化有抑制活性, 部分化合物活性比母体化合物Ebselen更优.

Synthesis and anti-lipid peroxidation activity of amino acid derivatives of benzisoselenazolone

Nine amino acid compounds (3～11) of benzoisoselenazolone were synthesized, where the phenyl ring at 2 position of 2-phenyl-1,2-benzoizoselenazol-3(2H)-one (Ebselen) with well-known antioxidative activity was replaced by ethyl aminoacetates. Effects of compounds 3～11 as well as Ebsene on Fe^2^+ / cysteine and vitamin C-induced rat liver microsome lipid peroxiation were investigated. Compounds 5,6 were more active than Ebselen in Fe^2^+ / cysteine system (Their IC~5~0 were 14,12 and 24μmol/L respectively ). And in vitamin C system, compound 4,7,8,9 and 10 were more active than Ebselen (Their IC~5~0 were 33,51,39,28,17.5 and 66μmol/L respectively) .