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1取代-1,2,4-三唑类化合物是一类广谱、高效、低毒、持效长的内吸性杀菌剂,同时三唑类杀菌剂单一的作用机制使真菌对这类化合物的抗性问题越来越突出,对三唑类杀菌剂的结构改造,修饰以克服抗性问题成为研究热点。本文试图对现有杀菌剂三唑酮、三唑醇、多效唑等进行结构修饰,改变分子的立体空间构象及亲脂性,用脂肪(杂)环取代苯氧基或苄基,设计并合成新的三唑类化合物Ⅱ1-8通过化合物Ⅱ1-8的生物活性的研究,试图说明以柔顺性较好的脂肪(杂)环取代钢性苯环后,对这类化合物活性的影响情况。
1 substituted -1,2,4-triazole compounds are a class of broad-spectrum, high efficiency, low toxicity, long-lasting systemic fungicide, and a single mechanism of action of fungicides triazoles fungi on these compounds The problem of resistance has become more and more prominent. The structural modification and modification of triazole fungicides have become the research hotspot. In this paper, we try to modify the existing fungicides such as triadimefon, triadimenol and paclobutrazol, change the stereospecific conformation and lipophilicity of the molecule, replace the phenoxy or benzyl group with aliphatic (hetero) rings, and design and synthesize new Triazole compounds Ⅱ1-8 through the biological activity of compound Ⅱ 1-8, trying to illustrate the flexibility of the fat (hetero) ring instead of steel benzene ring on the activity of these compounds.