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

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

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R1取代对其生物活性有较大的影响 ,当R1=(CH3 ) 3 C时 ,对小麦锈病的抑制活性要高于R1=Ar的活性 。

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.