National Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, China.
J Agric Food Chem. 2024 Mar 20;72(11):5585-5594. doi: 10.1021/acs.jafc.3c06696. Epub 2024 Mar 5.
To find novel nematicides, we screened the nematicidal activity of compounds in our laboratory compound library. Interestingly, the compound -((1,2)-2-(2-fluoro-4-(trifluoromethyl)phenyl)cyclopropyl)-2-(trifluoromethyl)benzamide () showed a broad spectrum and excellent nematicidal activity. The LC values of compound against second-stage juveniles of (), , and are 1.30, 1.63, and 0.72 mg/L, respectively. Nematicidal activities of compound against second-stage juveniles of were 87.66% at 100 mg/L. Meanwhile, compound can not only observably inhibit the feeding, reproduction, and egg hatching of but can also effectively promote the oxidative stress adverse reactions of nematodes and cause intestinal damage. Compound can promote the production of MDA and inhibit the activities of defense enzymes SOD and GST in . Compound can affect the transcription of genes involved in regulating the tricarboxylic acid cycle in nematodes, resulting in weakened nematode respiration and reduced nematode activity and even death. In addition, compound had good inhibitory activity against five pathogenic fungi. Among them, the EC of compound against was 8.4 mg/L. In the future, we will devote ourselves to the toxicological and structural optimization research of the candidate nematicide .
为了寻找新型杀线虫剂,我们筛选了实验室化合物库中的化合物的杀线虫活性。有趣的是,化合物-((1,2)-2-(2-氟-4-(三氟甲基)苯基)环丙基)-2-(三氟甲基)苯甲酰胺()表现出广谱和优异的杀线虫活性。化合物对 ()、()和()的二龄幼虫的 LC 值分别为 1.30、1.63 和 0.72mg/L。化合物在 100mg/L 时对二龄幼虫的杀线虫活性为 87.66%。同时,化合物不仅可以明显抑制线虫的取食、繁殖和卵孵化,还可以有效促进线虫氧化应激不良反应,导致肠道损伤。化合物可以促进 MDA 的产生,并抑制线虫中防御酶 SOD 和 GST 的活性。化合物可以影响参与调节线虫三羧酸循环的基因的转录,导致线虫呼吸减弱,线虫活性降低,甚至死亡。此外,化合物对五种致病真菌具有良好的抑制活性。其中,化合物对 的 EC 值为 8.4mg/L。在未来,我们将致力于候选杀线虫剂的毒理学和结构优化研究。