College of Agriculture, Liaocheng University, Liaocheng 252000, P. R. China.
College of Chemistry and Chemical Engineering, Liaocheng University, Liaocheng 252000, P. R. China.
J Agric Food Chem. 2021 Sep 29;69(38):11470-11484. doi: 10.1021/acs.jafc.1c01346. Epub 2021 Sep 20.
The development of new green fungicides based on the structural optimization of natural products can effectively solve the problems of low safety and high pathogen resistance of traditional fungicides. In this paper, based on pyrazole amide compound with excellent fungicidal activity discovered in the previous work, a series of l-serine-derived pyrazole amide and waltherione alkaloid-derived pyrazole ester derivatives were synthesized. The structures were successively identified by H NMR, C NMR, high-resolution mass spectrometry, and X-ray single-crystal diffraction. The in vitro and in vivo fungicidal activity screening demonstrated that compound showed a good inhibition rate against . A transmission electron microscope and fluorescence microscope observation further revealed that compound may cause damage to the cell membranes and vacuoles, and the hyphae treated with could produce obvious and easily observed blue fluorescence. The succinate dehydrogenase (SDH) enzymatic activity and molecular docking simulation indicated that compounds and may be potential SDH inhibitors against sp
基于天然产物结构优化的新型绿色杀菌剂的发展可以有效解决传统杀菌剂安全性低、病原菌抗药性高的问题。本文在前人工作中发现具有优异杀菌活性的吡唑酰胺化合物的基础上，合成了一系列 l-丝氨酸衍生的吡唑酰胺和麦角硫因衍生的吡唑酯衍生物。结构通过 H NMR、C NMR、高分辨率质谱和 X 射线单晶衍射得到了确证。体外和体内杀菌活性筛选表明，化合物 对 表现出良好的抑制率。透射电子显微镜和荧光显微镜观察进一步表明，化合物 可能导致细胞膜和液泡受损，用 处理的菌丝会产生明显且易于观察的蓝色荧光。琥珀酸脱氢酶（SDH）酶活性和分子对接模拟表明，化合物 和 可能是潜在的 SDH 抑制剂，对 有抑制作用。
