Developing and excavating new agrochemicals with highly active and safe is an important tactic for protecting crop health and food safety. In this paper, to discover the new bactericide candidates, we designed, prepared a new type of 1,2,3,4-tetrahydro--carboline (THC) derivatives and evaluated the and bioactivities against the pv. (), pv. (), and pv. (). The bioassay results exhibited that most title molecules possessed good activity toward the three plant pathogenic bacteria, the compound A showed the most active against and with EC values of 7.27 and 4.89 mg mL respectively, and compound A exhibited the best inhibitory activity against with EC value of 4.87 mg mL. Pot experiments showed that compound A exhibited excellent antibacterial activities to manage rice bacterial leaf blight and citrus bacterial canker, with protective efficiencies of 52.67 and 79.79% at 200 mg mL, respectively. Meanwhile, compound A showed good control efficiency (84.31%) against kiwifruit bacterial canker at 200 mg mL. Antibacterial mechanism suggested that these compounds could interfere with the balance of the redox system, damage the cell membrane, and induce the apoptosis of cells. Taken together, our study revealed that tetrahydro--carboline derivatives could be a promising candidate model for novel broad-spectrum bactericides.

中文翻译：

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作为治疗细菌感染的细胞凋亡引发剂的新型四氢-β-咔啉衍生物的发现和构效关系研究

开发和挖掘高活性、安全的新型农用化学品是保护农作物健康和食品安全的重要策略。在本文中，为了发现新的候选杀菌剂，我们设计、制备了一种新型的1,2,3,4-四氢咔啉（THC）衍生物，并评估了其对细菌的生物活性。 ()，PV。 () 和 pv。 ()。生测结果表明，大多数标题分子对3种植物病原菌均具有良好的活性，其中化合物A的活性最强，EC值分别为7.27和4.89 mg·mL，化合物A的抑制活性最好，EC值分别为7.27和4.89 mg·mL。 4.87 毫克毫升。盆栽实验表明，化合物A对水稻白叶枯病和柑橘细菌性溃疡病表现出优异的抗菌活性，在200 mg·mL-1浓度下，保护效率分别为52.67%和79.79%。同时，化合物A在200 mg·mL-1浓度下对猕猴桃细菌性溃疡病表现出良好的防效（84.31%）。抗菌机制表明这些化合物可干扰氧化还原系统的平衡，损伤细胞膜，诱导细胞凋亡。综上所述，我们的研究表明四氢咔啉衍生物可能是新型广谱杀菌剂的有前途的候选模型。