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 B16 was the optimal active molecule, giving the EC50 values of 3.11 (Xanthomonas oryzae pv. oryzae), 3.20 (Xanthomonas axonopodis pv. citri) and 3.54 μg/mL (Pseudomonas syringae pv. actinidiae). Pot experiments revealed compound B16 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-醇修饰的咔唑衍生物的设计、合成和评价


由于快速增长的人口的需求，世界范围内需要高产和高质量的谷物。然而，由某些顽固的植物病原菌引起的疾病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疗效有限。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价了它们的杀菌活性。其中化合物 B16 是最佳活性分子，EC50 值为 3.11 （Xanthomonas oryzae pv. oryzae） 、 3.20 （Xanthomonas axonopodis pv. citri） 和 3.54 μg/mL （Pseudomonas syringae pv. actinidiae）。盆栽实验表明，化合物 B16 能够控制水稻细菌性叶枯病。一些生化分析表明，我们设计的化合物会破坏细菌细胞膜的完整性，从而导致细胞内蛋白质泄漏。这些发现可作为设计新型膜靶向抗菌剂治疗顽固植物细菌病害的参考。