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有机化学
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有机化学 ›› 2009, Vol. 29 ›› Issue (01): 94-99. 上一篇    下一篇

研究简报

2-(2’,6’-二氯苯基)-1,3-噻唑烷-4-酮衍生物的微波促进合成及抗真菌、 抗肿瘤活性研究

陈 华*,a; 白 洁a ; 赵 莲a ; 苑香果a ; 李小六*,a,b ; 曹克强c   

  1. (a河北大学化学与环境科学学院 河北省化学生物学重点实验室 保定 071002)
    (b河北大学化学与环境科学学院 教育部药物化学与分子诊断省部共建重点实验室 保定 071002)
    (c河北农业大学植物保护学院 保定 071001)
  • 收稿日期:2008-04-25 修回日期:2008-05-15 发布日期:2009-01-20
  • 通讯作者: 陈 华;李小六

Microwave Assisted Synthesis and Antifungal, Anti-tumor Study of 2-(2,6-Dichlorophenyl)-1,3-thiazolidin-4-ones

Chen, Hua*,a; Bai, Jie a; Zhao, Liana; Yuan, Xiangguoa;
Li, Xiaoliu*,a,b; Cao, Keqiangc
  

  1. (a Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Enviromental Science,
    Hebei University, Baoding 071002)
    (b Key Laboratory of Medicinal Chemistry and Molecular Diagnosis, Ministry of Education, College of Chemistry and Envi-romental Science, Baoding 071002)
    (c College of Plant Protection, Hebei Agricultural University, Baoding 071002)
  • Received:2008-04-25 Revised:2008-05-15 Published:2009-01-20
  • Contact: Chen, Hua;Li, Xiaoliu

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利用微波促进的方法, 以2,6-二氯苯甲醛、胺和巯基乙酸为原料, 合成了系列N-3位不同取代基团的噻唑烷酮衍生物. 部分化合物在Lawesson试剂作用下, 合成了其系列噻唑烷4-硫酮衍生物. 所有化合物通过IR, 1H NMR, MS和元素分析等方法确定结构. 测试了化合物对黄瓜白粉病菌的抑制活性和对宫颈癌细胞的毒性作用, 部分化合物表现出较好的生物活性.

关键词: 细胞毒性
, 微波合成, 噻唑烷-4-酮, 抗菌

A series of thiazolidin-4-ones with different group on the position N-3 were synthesized by a three-component cyclocondensation of 2,6-dichlorobenzaldehyde, amines and 2-mercaptoacetic acid using a microwave-assisted method. Some corresponding thiazolidin-4-thione derivatives were also prepared in the presence of Lawesson’s reagent. The structures of the synthesized compounds were confirmed by IR, 1H NMR, MS and elemental analysis. Antifungal (Sphaerotheca fusca Blum.) and cytotoxic activities against Hela cell of the compounds were evaluated, and some compounds showed good biological activities.

Key words: thiazolidin-4-one, antifungal, cytotoxic activity, microwave-assisted synthesis