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化学学报
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化学学报 ›› 2002, Vol. 60 ›› Issue (7): 1303-1310. 上一篇    下一篇

研究论文

α-(1H-1,2,4-三唑-1-基)-β-芳硫基取代苯酮的合成及生物活性研究

陈文彬;张耀谋;金桂玉   

  1. 南开大学元素有机化学研究所.天津(300071)
  • 发布日期:2002-07-15

Studies on Synthesis and Biological Activities of α-(1H-1,2,4- Triazol-1-yl)-β-Arylthioethyl Substituted Phenyl Ketones

Chen Wenbin;Zhang Yaomou;Jin Guiyu   

  1. State Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry, Nankai University.Tianjin(300071)
  • Published:2002-07-15

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利用2-（1H-1，2，4-三唑-1-基）-2-丙烯-1-酮（2）与取代硫酚或含巯基的 杂环化合物进行1，4-亲核加成，得到目标化合物3，其结构经元素分析、核磁和红 外光谱所证实，并对其进行了生物活性的测试，发现大部分化合物具有很好的抑菌 活性。结构与活性的关系表明不同的R~1取代对其生物活性有较大的影响，当R~1 = （CH_3）_3C时，对小麦锈病的抑制活性要高于R~1 = Ar的活性，而Ar上不同的 取代基对其活性影响不大。

关键词: 三唑 P, 亲核反应, 加成反应, 生物活性, 丙烯酮, 硫酚

The title compounds (3) have been prepared by 1,4-nucleophilic addition of 2-(1H-1,2,4-triazol-1-yl)-2-propen-1-one with substituted thiophenol or heterocyclic compounds containing mercapto group. Structures of these compounds were characterized by elemental analysis, ~1H NMR and IR spectral data. The results of biological evaluation reveal that most of the compounds possess good fungicidal activities. The study of the relationship of structure and activity indicates that substituent R~1 has significant effect on biological activities of the compounds. Compounds 3 exhibit higher activity against Puccinia recondita in wheat when R~1 is (CH_3)_3C, than when R~1 is Ar, while the substituents on group Ar have little effect on activities.

Key words: PYRRODIAZOLE P, NUCLEOPHILIC REACTION, ADDITION REACTION, BIOLOGICAL ACTIVITY, PROPENONE, THIOPHENOLS

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