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Ebselen氨基酸衍生物的合成及抗脂质过氧化作用 被引量:25

The Synthesis and Anti-lipid Peroxidation Activity of Amino Acid Derivatives of Ebselen
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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.
机构地区 武汉大学化学系
出处 《高等学校化学学报》 SCIE EI CAS CSCD 北大核心 1996年第6期914-916,共3页 Chemical Journal of Chinese Universities
关键词 脂质过氧化 苯并异硒唑酮 有机硒化合物 Ebselen,Benzisoselenazolone,Amino acid derivatives,Synthesis,Lipid peroxidation
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  • 1田少雷,药学学报,1993年,28卷,870页
  • 2孙士勇,中国医学科学院学报,1993年,15卷,58页
  • 3王夔,生命科学中的微量元素,1991年

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