Grain of high yield and quality is needed worldwide due to the needs of a rapidly increasing human population. However, diseases caused by some stubborn types of phytopathogenic bacteria can limit the health and yields of crops. Even worse, conventional commercial bactericides have limited efficacy against such diseases. Therefore, exploring some efficacious bactericidal alternatives is urgently needed. In this work, a new type of 3-(piperazin-1-yl)propan-2-ol modified carbazole derivatives was synthesized and assessed for their bactericidal activity. Among them, compound was the optimal active molecule, giving the EC values of 3.11 ( pv. ), 3.20 ( pv. ) and 3.54 μg/mL ( pv). Pot experiments revealed compound to be able to control rice bacterial leaf blight. Some biochemical assays illustrated that our designed compounds could destroy the integrality of bacterial cell membranes and thereby leading to leaking the intracellular protein. These findings may be regard as a reference for the design of novel membrane-targeting antimicrobial agents for managing stubborn plant bacterial diseases.

中文翻译：

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靶向细菌膜的新型3-(哌嗪-1-基)丙-2-醇修饰咔唑衍生物的设计、合成和评估


由于人口迅速增长的需求，全世界都需要高产和优质的谷物。然而，由一些顽固类型的植物病原细菌引起的疾病可能会限制作物的健康和产量。更糟糕的是，传统的商业杀菌剂对此类疾病的功效有限。因此，迫切需要探索一些有效的杀菌替代品。在这项工作中，合成了一种新型的3-(哌嗪-1-基)丙-2-醇改性咔唑衍生物并评估了其杀菌活性。其中，化合物是最佳活性分子，其 EC 值为 3.11 ( pv. )、3.20 ( pv. ) 和 3.54 μg/mL ( pv. )。盆栽实验表明该化合物能够控制水稻白叶枯病。一些生化测定表明，我们设计的化合物可以破坏细菌细胞膜的完整性，从而导致细胞内蛋白质泄漏。这些发现可被视为设计用于治疗顽固植物细菌性疾病的新型膜靶向抗菌剂的参考。