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.
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