Liu Mengting, Li Zhurui, Zhou Yue, Li Chengpeng, Chen Danping, Ouyang Guiping, Li Yan, Li Chenchen, Wang Zhenchao
College of Pharmacy, Guizhou Engineering Laboratory for Synthetic Drugs, Guizhou University, Guiyang, China.
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, China.
Pest Manag Sci. 2025 Sep;81(9):5092-5102. doi: 10.1002/ps.8864. Epub 2025 May 4.
Xanthomonas oryzae pv. oryzae (Xoo) is widely acknowledged as a highly destructive bacterial pathogen responsible for bacterial leaf blight (BLB), leading to substantial yield and economic losses in rice cultivation. This study involved the synthesis of 21 novel structural derivatives of 1-H-indole-3-pyrazole-mercaptoacetamide, followed by the assessment of their antibacterial properties.
The majority of the compounds under investigation exhibited inhibitory effects against Xoo. Notably, compound 7 demonstrated superior in vitro inhibitory potency against Xoo with a median effective concentration (EC) value of 2.57 μg mL, outperforming Thiodiazole copper (TC) (63.95 μg mL) and Bismerthiazol (BT) (61.46 μg mL). In glasshouse settings, compound 7 displayed therapeutic efficacy (76.36%) and protective efficacy (88.02%) against rice bacterial leaf blight. Additionally, compound 7 attenuated biofilm formation and extracellular polysaccharide secretion by Xoo, and disrupted the cell membrane, thereby impeding bacterial proliferation. Transcriptomic analysis indicated that differentially expressed genes were predominantly associated with the bacterial type VI secretion system, biotin metabolism, the two-component system, bacterial chemotaxis and flagellar assembly.
This study presents a promising 1-H-indole-3-pyrazole-mercaptoacetamide compound as a novel antibacterial approach. Compound 7 manifests inhibitory actions on Xoo growth by disrupting bacterial flagella assembly, biotin synthesis, the two-component system and the type VI secretion system, showcasing substantial potential for novel antibacterial agent development. © 2025 Society of Chemical Industry.
水稻白叶枯病菌（Xanthomonas oryzae pv. oryzae，Xoo）被广泛认为是一种极具破坏性的细菌病原体，可引发水稻白叶枯病，给水稻种植带来巨大的产量和经济损失。本研究合成了21种新型结构的1-H-吲哚-3-吡唑-巯基乙酰胺衍生物，并对其抗菌性能进行了评估。
大多数被研究的化合物对Xoo表现出抑制作用。值得注意的是，化合物7对Xoo表现出卓越的体外抑制效力，其半数有效浓度（EC）值为2.57μg/mL，优于噻菌铜（TC）（63.95μg/mL）和噻霉酮（BT）（61.46μg/mL）。在温室环境中，化合物7对水稻白叶枯病显示出治疗效果（76.36%）和保护效果（88.02%）。此外，化合物7减弱了Xoo的生物膜形成和胞外多糖分泌，并破坏了细胞膜，从而阻碍细菌增殖。转录组分析表明，差异表达基因主要与细菌VI型分泌系统、生物素代谢、双组分系统、细菌趋化性和鞭毛组装有关。
本研究提出了一种有前景的1-H-吲哚-3-吡唑-巯基乙酰胺化合物作为新型抗菌方法。化合物7通过破坏细菌鞭毛组装、生物素合成、双组分系统和VI型分泌系统对Xoo生长表现出抑制作用，展现出新型抗菌剂开发的巨大潜力。© 2025化学工业协会。
