| 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 |
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| 引用本文： | 陈华,苑香果,郭在红,赵莲,李小六,张金超.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[J].河北大学学报(自然科学版),2009,29(2):153. |
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| 作者姓名： | 陈华 苑香果 郭在红 赵莲 李小六 张金超 |
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| 作者单位： | 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 |
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| 基金项目： | 国家自然科学基金，河北省自然科学基金，中国博士后科学基金 |
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| 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.
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| 关 键 词： | 微波合成 噻唑烷酮 细胞毒性 糖苷酶抑制活性 |
Microwave Assisted Synthesis and Biological Activity of 2-(Hydroxymethyl)-3-aryl-1,3-thiazolidin-4-ones |
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| CHEN Hua,YUAN Xiang-guo,GUO Zai-hong,ZHAO Lian,LI Xiao-liu,ZHANG Jin-chao.Microwave Assisted Synthesis and Biological Activity of 2-(Hydroxymethyl)-3-aryl-1,3-thiazolidin-4-ones[J].Journal of Hebei University (Natural Science Edition),2009,29(2):153. |
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| Authors: | CHEN Hua YUAN Xiang-guo GUO Zai-hong ZHAO Lian LI Xiao-liu ZHANG Jin-chao |
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| Institution: | Laboratory of Chemical Biology;College of Chemistry and Environmental Science;Hebei University;Baoding 071002;China |
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| Abstract: | 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(α-amylase,α-and β-glucosidase) inhibitory activities and cytotoxic activity against Hela cell of the compounds 5 were also evaluated. |
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| Keywords: | microwave-assisted synthesis 1 3-thiazolidin-4-ones cytotoxic activity glycosidases inhibitory activitites |
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