State Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemical of Guizhou University, Huaxi District Guiyang 550025, China.
The Key Laboratory of Chemical Synthesis and Environmental Pollution Control-Remediation Technology of Guizhou Province, Xingyi Normal University for Nationalities, Xingyi 562400, China.
J Agric Food Chem. 2024 Jun 5;72(22):12434-12444. doi: 10.1021/acs.jafc.3c09928. Epub 2024 May 22.
A series of novel isoindoline-1-one derivatives containing piperidine moiety were designed and synthesized using natural compounds as raw materials, and their biological activities were tested for three bacterial and three fungal pathogens. These derivatives exhibited good against phytopathogenic bacteria activities against pv () and pv (). Some compounds exhibited excellent antibacterial activities against pv (). The dose of against (the maximum half lethal effective concentration (EC) = 21.3 μg/mL) was better than that of the thiediazole copper dose (EC = 53.3 μg/mL). Excitingly, further studies have shown that the molecular docking of with 2FBW indicates that it can fully locate the interior of the binding pocket through hydrogen bonding and hydrophobic interactions, thereby enhancing its anti- activity. Scanning electron microscopy (SEM) studies revealed that induced the cell membrane collapse. Moreover, the proteomic results also indicate that may be a multifunctional candidate as it affects the formation of bacterial biofilms, thereby exerting antibacterial effects.
一系列含有哌啶结构单元的新型异吲哚啉-1-酮衍生物被设计和合成,使用天然化合物作为原料,并对三种细菌和三种真菌病原体进行了生物活性测试。这些衍生物表现出对植物病原菌的良好活性,对 pv ()和 pv ()有抑制作用。一些化合物对 pv ()表现出优异的抗菌活性。化合物 对 的剂量(最大半致死有效浓度 (EC) = 21.3 μg/mL)优于噻二唑铜的剂量(EC = 53.3 μg/mL)。令人兴奋的是,进一步的研究表明,化合物 与 2FBW 的分子对接表明,它可以通过氢键和疏水相互作用完全定位在结合口袋的内部,从而增强其抗 活性。扫描电子显微镜 (SEM) 研究表明,化合物 诱导 细胞膜崩溃。此外,蛋白质组学结果也表明,化合物 可能是一种多功能候选药物,因为它影响细菌生物膜的形成,从而发挥抗菌作用。