Wang Jiali, Shi Haoran, Lu Aidang
School of Chemical Engineering and Technology, Hebei University of Technology, Tianjin 300401, China.
J Fungi (Basel). 2024 Feb 19;10(2):160. doi: 10.3390/jof10020160.
Plant diseases caused by pathogenic fungi or oomycetes seriously affect crop growth and the quality and yield of products. A series of novel 1,2,4-triazole derivatives containing carboxamide fragments based on amide fragments widely used in fungicides and the commercialized mefentrifluconazole were designed and synthesized. Their antifungal activities were evaluated against seven kinds of phytopathogenic fungi/oomycete. Results showed that most compounds had similar or better antifungal activities compared to mefentrifluconazole's inhibitory activity against , especially compound (92%), which possessed outstanding activity. Compound (EC = 13.095 μg/mL) showed a better effect than that of mefentrifluconazole (EC = 39.516 μg/mL). Compound (90%) displayed outstanding anti-oomycete activity against , with an EC value of 17.362 μg/mL, far superior to that of mefentrifluconazole (EC = 75.433 μg/mL). The result of molecular docking showed that compounds and possessed a stronger affinity for 14α-demethylase (CYP51). This study provides a new approach to expanding the fungicidal spectrum of 1,2,4-triazole derivatives.
由致病真菌或卵菌引起的植物病害严重影响作物生长以及产品的质量和产量。基于广泛用于杀菌剂的酰胺片段和商业化的联苯三唑醇,设计并合成了一系列含有羧酰胺片段的新型1,2,4-三唑衍生物。评估了它们对七种植物病原真菌/卵菌的抗真菌活性。结果表明,与联苯三唑醇对……的抑制活性相比,大多数化合物具有相似或更好的抗真菌活性,尤其是化合物……(92%),其具有出色的活性。化合物……(EC = 13.095 μg/mL)显示出比联苯三唑醇(EC = 39.516 μg/mL)更好的效果。化合物……(90%)对……表现出出色的抗卵菌活性,EC值为17.362 μg/mL,远优于联苯三唑醇(EC = 75.433 μg/mL)。分子对接结果表明,化合物……和……对14α-脱甲基酶(CYP51)具有更强的亲和力。本研究为拓宽1,2,4-三唑衍生物的杀菌谱提供了一种新方法。