THE SYNTHESIS AND ANTI-LIPID PEROXIDATION ACTIVITY OF AMINO-ACID DERIVATIVES OF EBSELEN

Amino acid was used as a carrier of the active molecule - ebselen, whi ch mimicked the properties of GSH-Px and was known as an anti-inflamma tory drug. Eight ebselen derivatives with amino acid ethyl esters atta ched to the p-position of 2-phenyl moiety were prepared. -Carboxylphen yl)-1,2-benzisoselenazol-3(2H)-one(1) was used as the intermediate pre pared in good yield by cyclization of 2-chloroselenobenaoyl chloride w ith 4-amino benzoic acid in the presence of Et(3)N. Then 1 was treated with p-toluenesulfonates of amino acid ethyl ester, and the target co mpounds were obtained by further purification. Effects of compounds 1, 2,3,4 as well as ebselen on Fe2+/cysteine-induced rat liver microsomal peroxidation were studied. Their IC50 were 30,22. 7,17., 7,22. 2 and 24 mu mol . L(-1), respectively.