The increasing resistance problems of pathogens have drastically reduced the efficiency of existing drugs and agricultural chemicals, increasing the difficulty of preventing and controlling bacterial diseases. To create effective bactericide alternatives, a series of novel 3-(piperazin-1-yl)propan-2-ol decorated carbazole derivatives was fabricated, and their bioactivities and drug-likeness properties were evaluated. The in vitro bioassays showed that target molecules had outstanding antibacterial activity against Xanthomonas oryzae pv. oryzae (Xoo), Xanthomonas axonopodis pv. citri (Xac), and Pseudomonas syringae pv. actinidiae (Psa), with optimal EC₅₀ values of 6.80 μg/mL (A₉), 6.37 μg/mL (A₉), and 10.75 μg/mL (A₁₀), respectively. Furthermore, a series of biochemical assays indicated that title molecules could negatively impact the function of bacteria by irreversibly damaging their cell membranes, resulting in cytoplasmic components leakage (nucleic acids and proteins). In addition, phytotoxicity test and in silico toxicity predictions suggested that compound A₉ had low phytotoxicity, and possessed acceptable drug-like properties. Our results showed that carbazole derivatives containing an 3-(piperazin-1-yl)propan-2-ol moiety were promising skeletons to develop novel bactericides with low toxicity for controlling refractory microbial diseases by targeting cell membranes.

病原体的耐药性问题日益严重，大大降低了现有药物和农药的效率，增加了预防和控制细菌性疾病的难度。为了创造有效的杀菌剂替代品，制备了一系列新型 3-(piperazin-1-yl)propan-2-ol 修饰的咔唑衍生物，并评估了它们的生物活性和类药特性。体外生物测定表明目标分子对米黄单胞菌光伏具有突出的抗菌活性。oryzae ( Xoo ), Xanthomonas axonopodis pv。柑橘( Xac ) 和Pseudomonas syringae pv。猕猴桃( Psa )，最佳 EC ₅₀值分别为 6.80 μg/mL ( A ₉ )、6.37 μg/mL ( A ₉ ) 和 10.75 μg/mL ( A ₁₀ )。此外，一系列生化分析表明，标题分子可能通过不可逆地破坏细菌的细胞膜而对细菌的功能产生负面影响，从而导致细胞质成分泄漏（核酸和蛋白质）。此外，植物毒性试验和计算机毒性预测表明化合物A ₉具有低植物毒性，并具有可接受的药物样特性。我们的研究结果表明，含有 3-(piperazin-1-yl)propan-2-ol 部分的咔唑衍生物是开发具有低毒性的新型杀菌剂的有前途的骨架，用于通过靶向细胞膜来控制难治性微生物疾病。