含嘧啶氨基的三氨基取代三嗪衍生物的设计、合成及抗苹果树腐烂病菌活性

依据三嗪和嘧啶衍生物的抗菌特性以及生物活性叠加原理, 以三聚氯氰为起始原料, 设计、合成了系列新的含嘧啶氨基的2,4,6-三氨基取代-1,3,5-三嗪化合物. 化合物的结构经1H NMR, ESI-MS和元素分析等表征. 化合物的抗苹果树腐烂病菌活性测试结果表明, 大部分化合物对苹果树腐烂病菌具有显著的抑制作用, 如化合物2aa, 2ba, 2ca, 2da, 3ba和3ea在200 μg/mL浓度下的抑制率分别为96.33%, 98.17%, 97.25%, 97.71%, 98.39%和94.50%, 在100 μg/mL浓度下的抑制率也均在74%以上.

Design, Synthesis and Antifungal Activity Against Valsa Mali of the Triamino Substitued Triazines Bearing Aminopyrimidine Group

In order to find novel plant fungicides targeting Valsa mali with high activity, fifteen triamino substituted 1,3,5-triazine compounds bearing 2-amino-4,6-dimethyl-5-(un) substituted pyrimidine were designed according to the antifungal characteristics of triazine and pyrimidine and the superposition principle of reinforcement of biological activity. These compounds were synthesized by amino substitution using cyanuric chloride as the starting material, and their structures were characterized and determined by 1H NMR, ESI-MS and elemental analysis. The antifungal activity against Valsa mali of the new compounds were evaluated and the results showed that a majority of the compounds have notable inhibitory activity against Valsa mali. For examples, at the concentration of 200 μg/mL, compounds 2aa, 2ba, 2ca, 2da, 3ba and 3ea have the  inhibition rate of 96.33%, 98.17%, 97.25%, 97.71%, 98.39% and 94.50%, respectively, and have the inhibition rates above 74% at the concentration of 100 μg/mL, which suggest that such triamino substituted triazine compounds have the potential applications in further development for new fungicides.