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Design, synthesis and antimicrobial activity evaluation of novel Marinoquinoline derivatives against phytopathogenic bacteria
Pest Management Science ( IF 3.8 ) Pub Date : 2024-12-28 , DOI: 10.1002/ps.8609
Han Zhou, Deng‐Tuo Wang, Li Ma, Ya‐Rui Jin, Lu‐Lu Qin, Tian‐Li Dai, Yue Zhang, Wen Zhang, Zhi‐Jun Zhang, Shao‐Yong Zhang, Gui‐Sha Chen, Guo‐Liang Mou, Ying‐Qian Liu
Pest Management Science ( IF 3.8 ) Pub Date : 2024-12-28 , DOI: 10.1002/ps.8609
Han Zhou, Deng‐Tuo Wang, Li Ma, Ya‐Rui Jin, Lu‐Lu Qin, Tian‐Li Dai, Yue Zhang, Wen Zhang, Zhi‐Jun Zhang, Shao‐Yong Zhang, Gui‐Sha Chen, Guo‐Liang Mou, Ying‐Qian Liu
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BACKGROUNDPlant diseases caused by plant pathogens pose a great threat to biodiversity and food security, and the problem of drug resistance caused by traditional antibiotics and fungicides is becoming more and more serious. It is urgent to develop new antibacterial molecules with low toxicity and high efficiency. Marinoquinoline A is an alkaloid isolated from marine actinomycetes and has a variety of pharmacological activities. In this study, a series of compounds were designed and synthesized by fragment fusion strategy inspired by Marinoquinoline, and their antibacterial activities were evaluated, and the structure–activity relationship was discussed.RESULTSAmong these derivatives, ZM‐9 showed the most significant antibacterial activity against Xanthomonas oryzae (Xoo ) with MIC of 1.56 μg mL−1 , while ZN‐8 showed the best antibacterial activity against Xanthomonas axonopodis pv. Citri (Xac ) with MIC of 0.78 μg mL−1 , both of which were better than Thiodiazole copper. The results of in vivo antibacterial activity test showed that 200 μg mL−1 ZM‐9 and ZN‐8 had significant control effects on rice and citrus. The biochemical experiments showed that ZM‐9 and ZN‐8 could inhibit the secretion of extracellular polysaccharides, destroy the biofilm integrity of the pathogens, increase permeability, and cause oxidative stress damage.CONCLUSIONIn summary, most of the chemical entities inspired by Marinoquinoline have shown good antibacterial activity. In particular, compounds ZM‐9 and ZN‐8 can be used as lead compounds for further structural optimization to develop new antibacterial agents. © 2024 Society of Chemical Industry.
中文翻译:
针对植物病原菌的新型马里诺喹啉衍生物的设计、合成和抗菌活性评价
背景植物病原菌引起的病害对生物多样性和粮食安全构成巨大威胁,传统抗生素和杀菌剂引起的耐药问题越来越严重。迫切需要开发低毒、高效的新型抗菌分子。Marinoquinoline A 是一种从海洋放线菌中分离的生物碱,具有多种药理活性。本研究受 Marinoquinoline 启发,采用片段融合策略设计合成了一系列化合物,评价了它们的抗菌活性,并讨论了构效关系。结果在这些衍生物中,ZM-9 对米黄单胞菌 (Xoo) 表现出最显着的抗菌活性,MIC 为 1.56 μg mL-1,而 ZN-8 对轴孢黄单胞菌 pv 表现出最好的抗菌活性。MIC 为 0.78 μg mL-1 的 Citri (Xac),两者均优于硫二唑铜。体内抗菌活性试验结果表明,200 μg mL−1 ZM-9 和 ZN-8 对水稻和柑橘具有显著的控制作用。生化实验表明,ZM-9 和 ZN-8 可抑制细胞外多糖的分泌,破坏病原菌的生物膜完整性,增加通透性,并引起氧化应激损伤。结论综上所述,受 Marinoquinoline 启发的大多数化学实体都显示出良好的抗菌活性。特别是,化合物 ZM-9 和 ZN-8 可用作铅化合物,用于进一步结构优化以开发新的抗菌剂。© 2024 化工学会.
更新日期:2024-12-28
中文翻译:
![](https://scdn.x-mol.com/jcss/images/paperTranslation.png)
针对植物病原菌的新型马里诺喹啉衍生物的设计、合成和抗菌活性评价
背景植物病原菌引起的病害对生物多样性和粮食安全构成巨大威胁,传统抗生素和杀菌剂引起的耐药问题越来越严重。迫切需要开发低毒、高效的新型抗菌分子。Marinoquinoline A 是一种从海洋放线菌中分离的生物碱,具有多种药理活性。本研究受 Marinoquinoline 启发,采用片段融合策略设计合成了一系列化合物,评价了它们的抗菌活性,并讨论了构效关系。结果在这些衍生物中,ZM-9 对米黄单胞菌 (Xoo) 表现出最显着的抗菌活性,MIC 为 1.56 μg mL-1,而 ZN-8 对轴孢黄单胞菌 pv 表现出最好的抗菌活性。MIC 为 0.78 μg mL-1 的 Citri (Xac),两者均优于硫二唑铜。体内抗菌活性试验结果表明,200 μg mL−1 ZM-9 和 ZN-8 对水稻和柑橘具有显著的控制作用。生化实验表明,ZM-9 和 ZN-8 可抑制细胞外多糖的分泌,破坏病原菌的生物膜完整性,增加通透性,并引起氧化应激损伤。结论综上所述,受 Marinoquinoline 启发的大多数化学实体都显示出良好的抗菌活性。特别是,化合物 ZM-9 和 ZN-8 可用作铅化合物,用于进一步结构优化以开发新的抗菌剂。© 2024 化工学会.