【摘要】 在已知具有抗氧化作用的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Fe²⁺/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。更多还原

【Abstract】 Nine amino acid compounds (3-11) of benzoisoselenazolone were synthesized, where the phenyl ring at 2 position of 2-phenyl-1,2-benzoisoselenazol-3(2H)-one (Ebselen) with well-known antioxidative activity was replaced by ethyl aminoacetates. Effects of compounds 3- 11 as well as Ebselen on Fe2+/ cysteine and vitamin C-induced rat liver microsome lipid peroxidation were investigated. Compounds 5, 6 were more active than Ebselen in Fe2+ / cysteine system (Their IC50 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 IC50 were 33, 51, 39, 28, 17.5 and 66μmol / L respectively).更多还原