Metyltetraprole的合成及杀菌活性

Synthesis and fungicidal activity of metyltetraprole

[目的]合成metyltetraprole,并探究其在农业真菌防治中的潜在应用。[方法]以对氯碘苯、5-羟基吡唑和2-甲基-3-溴苯胺为原料合成metyltetraprole,采用活体盆栽试验测定其对黄瓜霜霉病、小麦白粉病、大豆锈病和大豆灰霉病的体外杀菌活性,并通过分子对接预测其抗真菌机制。[结果]Metyltetraprole在1.5625 mg/L质量浓度下对大豆锈病具有100%的防治效果;在6.25 mg/L的质量浓度下,对小麦白粉病防效为93%;在最高质量浓度100 mg/L下,对黄瓜霜霉病和大豆灰霉病的防治效果分别为100%和80%。分子对接结果表明,metyltetraprole与受体蛋白之间存在氢键、范德华力、π-π堆积、C-H、π-σ等相互作用。[结论]Metyltetraprole展现了广泛而良好的杀菌活性,为农业真菌防治领域的新药研发与应用提供了新的探索方向。

[Aims]The aim of this study is to synthesize metyltetraprole and explore its potential application in agricultural fungi control.[Methods]Methyltetraprole was synthesized using 4-chloroiodobenzene,5-hydroxypyrazole,and 3-bromo-2-methyl aniline as raw materials.The in vitro fungicidal activity of metyltetraprole against cucumber downy mildew,wheat powdery mildew,soybean rust and soybean gray mold was determined using the live plant pot test method.The fungicidal mechanism was evaluated through molecular docking.[Results]Metyltetraprole exhibited 100%control against soybean rust at a concentration of 1.5625 mg/L,and 93%control against wheat powdery mildew at 6.25 mg/L.The control efficacy against cucumber downy mildew and soybean gray mold at 100 mg/L was 100%and 80%respectively.Molecular docking results identified hydrogen bonds,van der Waals forces,π-πstacking,C-H interactions,andπ-o interactions between metyltetraprole and the receptor protein.[Conclusions]Methyltetraprole exhibits excellent broad-spectrum fungicidal activity,providing a novel direction for research and application in the field of agricultural fungi control.