Zhang Yong, Zhu Mei, Zhu Zongnan, Zou Yue, Liu Xing, Chen Jixiang
State 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, China.
Pest Manag Sci. 2025 Mar;81(3):1669-1682. doi: 10.1002/ps.8573. Epub 2024 Nov 26.
Bacterial diseases in plants pose a serious threat to crop production, leading to substantial food loss every year. Prolonged and repeated use of a single antibacterial agent can promote resistance in pathogenic bacteria. Therefore, there is an urgent need to develop efficient antibacterial agents for the treatment of bacterial diseases.
Sulfone derivatives containing an oxazole moiety were designed and synthesized. Subsequently, their biological activities were evaluated. The half-maximal effective concentration (EC) value of compound F10 against Xanthomonas oryzae pv. oryzicola (Xoc) was 1.1 mg/L, which was higher than those of commercial antibacterial agents, thiodiazole-copper (91.5 mg/L) and bismerthiazol (76.0 mg/L). The curative and protective effects of compound F10 against bacterial leaf streak in rice were 43.8% and 48.4%, respectively, at 200 mg/L, which were significantly superior to those of thiodiazole-copper (25.0% and 25.8%, respectively) and bismerthiazol (31.3% and 38.7%, respectively). Compound F10 inhibits Xoc by increasing the permeability of the cell membrane, inhibiting the production of extracellular polysaccharides, and affecting flagellar movement on the cell membrane. In addition, F10 reduces the pathogenicity of pathogenic bacteria, induces the accumulation of reactive oxygen species (ROS) in pathogenic bacteria, and produces adverse reactions. Compound F10 weakens bacterial pathogenicity by affecting the signal transduction of plant hormones, programmed cell death, and enhancing the ability to resist infection through the autoimmune response of rice.
Therefore, compound F10 can be used as a potential antibacterial agent in future applications. © 2024 Society of Chemical Industry.
植物细菌病害对作物生产构成严重威胁，每年导致大量粮食损失。长期反复使用单一抗菌剂会促使病原菌产生抗性。因此，迫切需要开发高效抗菌剂来治疗细菌病害。
设计并合成了含恶唑部分的砜衍生物。随后，对其生物活性进行了评估。化合物F10对水稻白叶枯病菌（Xoc）的半数有效浓度（EC）值为1.1毫克/升，高于市售抗菌剂噻菌铜（91.5毫克/升）和叶枯唑（76.0毫克/升）。在200毫克/升时，化合物F10对水稻细菌性条斑病的治疗和保护效果分别为43.8%和48.4%，显著优于噻菌铜（分别为25.0%和25.8%）和叶枯唑（分别为31.3%和38.7%）。化合物F10通过增加细胞膜通透性、抑制胞外多糖产生以及影响细胞膜上的鞭毛运动来抑制Xoc。此外，F10降低病原菌的致病性，诱导病原菌中活性氧（ROS）的积累并产生不良反应。化合物F10通过影响植物激素信号转导、程序性细胞死亡以及增强水稻自身免疫反应抵抗感染的能力来削弱细菌致病性。
因此，化合物F10在未来应用中可作为潜在的抗菌剂。© 2024化学工业协会。
