2-羟甲基-3-芳基-1,3-噻唑烷-4-酮衍生物的微波促进合成及生物活性  

Microwave Assisted Synthesis and Biological Activity of 2-(Hydroxymethyl)-3-aryl-1,3-thiazolidin-4-ones

作　　者：陈华[1] 苑香果[1] 郭在红[1] 赵莲[1] 李小六[1] 张金超[1] 

机构地区：[1]河北大学化学与环境科学学院化学生物学实验室,河北保定071002

出　　处：《河北大学学报（自然科学版）》2009年第2期153-159,共7页Journal of Hebei University(Natural Science Edition)

基　　金：国家自然科学基金资助项目(20672027);河北省自然科学基金资助项目(B2008000588);国家博士后基金资助项目

摘　　要：以乙醛酸乙酯、芳香胺及杂环胺和巯基乙酸为起始原料,利用微波促进多组分一锅法合成了系列新型噻唑烷酮衍生物(4),进一步经NaBH4还原得到新的2-羟甲基-3-芳基-1,3-噻唑烷-4-酮化合物(5).目标化合物结构通过1H NMR,13C NMR,MS等方法确定,并初步测试了化合物对糖苷酶(α-淀粉酶,α-和β-葡萄糖苷酶)及对宫颈癌细胞的抑制作用.A series of novel 2-（hydroxymethyl）-3-aryl-1,3-thiazolidin-4-ones （5） were conveniently synthesized by the microwave-assisted three-component one-pot condensation of glyoxylic acid ethyl, aromatic amines and 2-mercaptoacetic acid, which provided a series of new compounds of 1,3-thiazolidin-4- ones （4）, and followed by the reduction with NaBH4. The structures of the compounds 5 have been determined by 1H NMR,13C NMR and MS spectral analysis. The glycosidases （a-amylase, α- andβ-glucosidase） inhibitory activities and cytotoxic activity against Hela cell of the compounds 5 were also evaluated.

关 键 词：微波合成 噻唑烷酮 细胞毒性 糖苷酶抑制活性 

分 类 号：O621.3[理学—有机化学]