BackgroundA large number of pathogenic fungi have caused serious damage to the global crop yield, and drug resistance is always a topic that cannot be avoided for traditional fungicides. Therefore, finding efficient, green, and low‐toxic fungicides is our primary task, which brings opportunities for the development of natural product green pesticides.ResultsTwenty chalcone derivatives containing 1,2,3,4‐tetrahydroquinoline were designed and synthesized, and the compounds were tested for their fungicidal effects against eight plant pathogenic fungi in vitro. The results demonstrate that the original splicing did not have fungicidal activity, so a piperazine fragment was introduced; the test results revealed that H1–H10 all had good antifungal activity. Among them, H4 showed the highest inhibitory activity against Phytophthora capsici (Pc) with a median effect concentration (EC50) value of 5.2 μg/mL, which was higher than that of the control drugs Azoxystrobin (EC50 = 80.2 μg/mL) and Fluopyram (EC50 = 146.8 μg/mL). After the study, it was demonstrated that H4 mainly acted on the cell membrane against Phytophthora capsici and inhibited the activity of the marker enzyme of mitochondria (SDH) in the fungus.ConclusionH4 has significant resistance to Phytophthora capsici and also plays a significant role in inhibiting SDH activity, providing a new direction for the development of green pesticides. © 2024 Society of Chemical Industry.

中文翻译：

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含有 1,2,3,4-四氢喹啉的查耳酮衍生物的抗真菌活性及其作为潜在 SDH 抑制剂的研究


背景大量的病原真菌对全球农作物产量造成了严重损害，耐药性一直是传统杀菌剂无法回避的话题。因此，寻找高效、绿色、低毒的杀菌剂是我们的首要任务，这为天然产物绿色农药的开发带来了机遇。结果设计合成了 20 种含有 1,2,3,4-四氢喹啉的查耳酮衍生物，并在体外测试了这些化合物对 8 种植物病原真菌的杀菌作用。结果表明，原始剪接不具有杀真菌活性，因此引入了哌嗪片段;检测结果显示 H1-H10 均具有良好的抗真菌活性。其中，H4 对辣椒疫霉 （Pc） 的抑制活性最高，中位效应浓度 （EC50） 值为 5.2 μg/mL，高于对照药物嘧菌酯 （EC50 = 80.2 μg/mL） 和氟吡仑 （EC50 = 146.8 μg/mL）。研究结果表明，H4 主要作用于细胞膜对抗辣椒疫霉，并抑制真菌中线粒体标志物酶 （SDH） 的活性。结论H4 对辣椒疫霉具有显著的抗性，在抑制 SDH 活性方面也发挥重要作用，为绿色农药的发展提供了新的方向。© 2024 化工学会.