School of Pharmaceutical Sciences, Guizhou University, Guiyang 550025, 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 550025, China.
Int J Mol Sci. 2023 Jun 30;24(13):10900. doi: 10.3390/ijms241310900.
Rice bacterial leaf blight is a destructive bacterial disease caused by () that seriously threatens crop yields and their associated economic benefits. In this study, a series of improved dissolubility 7-aliphatic amine tryptanthrin derivatives was designed and synthesized, and their potency in antibacterial applications was investigated. Notably, compound exhibited excellent activity against , with an EC value of 2.55 μg/mL, compared with the positive control bismerthiazol (EC = 35.0 μg/mL) and thiodiazole copper (EC = 79.4 μg/mL). In vivo assays demonstrated that exhibited a significant protective effect on rice leaves. After exposure, the morphology of the bacteria was partially atrophied by SEM. Furthermore, increased the accumulation of intracellular reactive oxygen species, causing cell apoptosis and the formation of bacterial biofilms. All the results indicated that could be a potential agrochemical bactericide for controlling phytopathogenic bacteria.
水稻细菌性条斑病是一种由 ()引起的破坏性细菌性疾病，严重威胁作物产量和相关经济效益。在本研究中，设计并合成了一系列改良的 7-脂肪胺色胺酮衍生物，研究了它们在抗菌应用中的效力。值得注意的是，化合物 ()对表现出优异的抗菌活性，EC 值为 2.55μg/mL，优于阳性对照双脒噻唑 (EC = 35.0μg/mL) 和噻二唑铜 (EC = 79.4μg/mL)。体内试验表明， ()对水稻叶片表现出显著的保护作用。暴露后，扫描电子显微镜观察到细菌的形态部分萎缩。此外， ()增加了细胞内活性氧的积累，导致细胞凋亡和细菌生物膜的形成。所有结果表明， ()可能是一种潜在的农用杀菌剂，可用于防治植物病原菌。
