有机化学 ›› 2008, Vol. 28 ›› Issue (05): 894-898. 上一篇    下一篇

研究简报

芳醛-[5-(3,4,5-三甲氧基苯基)-1,3,4-噻二唑-2-巯基]-乙酰腙衍生物的合成及生物活性研究

陈江,刘芳,宋宝安*,杨松
胡德禹,金林红,陈卓,薛伟   

  1. (贵州大学精细化工研究开发中心 教育部绿色农药与农业生物工程重点实验室 贵阳 550025)
  • 收稿日期:2007-07-19 修回日期:2007-10-12 发布日期:2008-05-20
  • 通讯作者: 宋宝安

Synthesis and Bioactivity of Arylaldehyde-[5-(3,4,5-Trimethoxy- phenyl)-1,3,4-thiadiazol-2-yl]-thiol Acetyl Hydrazones

CHEN Jiang,LIU Fang,SONG Bao-An*,YANG Song
HU De-Yu,JIN Lin-Hong,CHEN Zhuo,XUE Wei   

  1. (Key Laboratory of Green Pesticide and Agriculture Bioengineering, Ministry of Education, Research and Development
    Center for Fine Chemicals, Guizhou University, Guiyang 550025)
  • Received:2007-07-19 Revised:2007-10-12 Published:2008-05-20
  • Contact: SONG Bao-An

采用活性基团拼接法, 以2-巯基-5-(3,4,5-三甲氧基苯基)-1,3,4-噻二唑为原料, 经硫醚化、肼解、腙化反应合成了8个芳醛-[5-(3,4,5-三甲氧基苯基)-1,3,4-噻二唑-2-巯基]-乙酰腙衍生物, 并经过元素分析, IR, 1H NMR, 13C NMR对其结构进行了确认. 初步生物活性测试表明, 部分化合物具有一定的抑菌生物活性.

关键词: 酰腙衍生物, 1,3,4-噻二唑, 合成, 抑菌活性

Eight arylaldehyde-[5-(3,4,5-trimethoxyphenyl)-1,3,4-thiadiazol-2-yl]-acetyl hydrazone derivatives were synthesized with [5-(3,4,5-trimethoxyphenyl)-1,3,4-thiadiazole-2-thiol as starting material according to substructure link principle, followed by thioetherification, hydrazide reaction and hydrazone reaction. The structures of these compounds were determined by elemental analysis, IR, 1H NMR, and 13C NMR spectra. Bioassay of the title compounds indicated that some of them exhibited moderate antifungal activity.

Key words: 1,3,4-thiadiazole, synthesis, antifungal activity, hydrazone derivative