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.