2-取代-4-芳基-2H-1,2,3-三唑类化合物的合成及杀菌活性

1,2,3-三唑化合物具有广泛的生物活性,为了发现具有杀菌活性的新型化合物分子结构,以芳醛、硝基甲烷及叠氮化钠为起始原料,合成了11个2-取代-4-芳基-2H-1,2,3-三唑类系列化合物,目标物的收率为51%~91%。核磁共振谱、质谱和元素分析等技术手段对目标化合物的结构经进行了表征。结果表明,在25 mg/L的测试质量浓度下,大部分化合物对小麦赤霉病菌及辣椒疫霉病菌显示出初步的抑菌活性,其中,化合物3a对小麦赤霉病菌的抑制率为80. 4%,化合物3b对黄瓜灰霉病菌为78. 2%,化合物3b及3h对油菜菌核病菌的抑制率分别70. 3%和75. 9%。

Synthesis and Fungicidal Activity of 2-Substituted-4-aryl-2H-1,2,3-triazole Derivatives

1,2,3-Triazole compounds show a wide range of biological activities. In order to find new compounds with bactericidal activity, a series of 2-substituted-4-aryl-2H-1,2,3-triazoles was synthesized from benzaldehyde or substituted benzaldehyde, nitromethane and sodium azide in 51% to 91% yields. The structures of these compounds were characterized by nuclear magnetic resonance spectroscopy(NMR), mass spectra and elemental analyses. Most of these compounds show the preliminary antibacterial activity against Gibberella zeae and Phytophythora capsici in vitro, in 25 mg/L concentration. Among them, compound 3a shows 80.4% activity of against Gibberella zeae, compound 3b shows 78.2% activity of against Botrytis cinerea, compounds 3a and 3h show 70.3%, 75.9% activities of against Sclerotonia sclerotiorum, respectively.