应用化学 ›› 2017, Vol. 34 ›› Issue (10): 1161-1171.DOI: 10.11944/j.issn.1000-0518.2017.10.170163

• 研究论文 • 上一篇    下一篇

含有苯磺酰胺基团1,2,4-三唑和噻二唑类化合物的设计、合成及抑菌活性

陈明桂a,华学文b,魏巍a,张冬凯a,刘明a,吴长春a,李玉新a,王宝雷a,周莎a,李正名a*()   

  1. a南开大学元素有机化学国家重点实验室,化学化工协同创新中心(天津) 天津 300071
    b聊城大学农学院 山东 聊城 252000
  • 收稿日期:2017-05-18 接受日期:2017-06-28 出版日期:2017-09-29 发布日期:2017-09-29
  • 通讯作者: 李正名
  • 基金资助:
    国家自然科学基金(21272129)项目资助

Design, Synthesis and Fungicidal Bioactivity of 1,2,4-Triazoles or Thiadiazoles Containing a Benzenesulfonamide Moiety

CHEN Mingguia,HUA Xuewenb,WEI Weia,ZHANG Dongkaia,LIU Minga,WU Changchuna,ZHOU Shaa,LI Yuxina,WANG Baoleia,ZHOU Shaa,LI Zhengminga*()   

  1. aState Key Laboratory of Elemento-Organic Chemistry,Collaborative Innovation Center of Chemical Science and Engineering(Tianjin),Nankai University,Tianjin 300071,China
    bCollege of Agriculture,Liaocheng University,Liaocheng,Shandong 252000,China
  • Received:2017-05-18 Accepted:2017-06-28 Published:2017-09-29 Online:2017-09-29
  • Contact: LI Zhengming
  • Supported by:
    Supported by the National Natural Science Foundation of China(No.21272129)

摘要:

为了探索高效低毒、环境友好的新型杀菌剂,本文设计合成系列含有苯磺酰胺片段的1,2,4-三唑和噻二唑类化合物。 所有目标化合物的结构由核磁共振波谱、质谱和元素分析确认。 离体抑菌活性测试结果表明,部分化合物对7种常见植物病原真菌表现出不同的抑制作用,其中化合物10a、10g和10n对水稻恶苗病菌的抑制活性较高为48.6%,接近商品化杀菌剂嘧菌酯(52.9%)。 以上结果可能为后续的分子设计提供依据。

关键词: 三唑, 噻二唑, 苯磺酰胺, 抑菌活性

Abstract:

In order to explore efficient, low toxic and eco-friendly fungicides, a series of 1,2,4-triazole and thiadiazole derivatives containing benzenesulfonamide moieties was designed and synthesized. Their chemical structures were confirmed by nuclear magnetic resonance spectroscopy(NMR), mass spectrometry and elemental analysis. Preliminary fungicidal bioassay in vitro was carried out against seven plant pathogenic fungi and the results showed that compounds 10 exhibited moderate fungicidal activities, especially 10a, 10g and 10n demonstrated similar high inhibition rate against Fusarium moniliforme in comparison with commercial Azoxystrobin.

Key words: triazole, thiadiazole, benzenesulfonamide, fungicidal activity