On the basis of the active substructure combination principle, 24 novel synthesis of novel bis-sulfoxide derivatives bearing acylhydrazone and benzothiazole moieties as potential antibacterial agents were designed and synthesized. The bioactivity assay results showed that many compounds had significant in vitro inhibitory effects against Xanthomonas oryzae pv. oryzae (Xoo) and Xanthomonas citri pv. citri (Xac). Notably, compound 4b had the best in vitro antibacterial activity against Xoo at an half-maximal effective concentration value of 11.4 μg/mL, which was superior to those of thiodiazole copper (TDC) and bismerthiazol (BMT). Compared with TDC and BMT, compound 4b was more effective in vivo controlling rice bacterial leaf blight with curative and protection activities of 42.5% and 40.3%, respectively. In addition, compound 4b can influence biofilm formation, inhibit extracellular polysaccharide production, and ultimately reduce the pathogenicity of Xoo. All the results indicated that bis-sulfoxide derivatives bearing acylhydrazone and benzothiazole moieties can be used for the development of small-molecule pesticides with high antibacterial activity.

中文翻译：

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发现具有酰腙和苯并噻唑部分的新型双亚砜衍生物作为潜在的抗菌剂

基于活性子结构组合原理，设计并合成了 24 种新型双亚砜衍生物，它们带有酰腙和苯并噻唑部分作为潜在的抗菌剂。生物活性测定结果表明，许多化合物在体外对米黄单胞菌有显着抑制作用。oryzae (Xoo) 和 Xanthomonas citri pv。柑橘 (Xac)。值得注意的是，化合物4b在11.4 μg/mL的半最大有效浓度值下对Xoo具有最佳体外抗菌活性，优于硫二唑铜（TDC）和双甲基噻唑（BMT）。与TDC和BMT相比，化合物4b在体内防治水稻白叶枯病的效果更好，治疗和保护活性分别为42.5%和40.3%。此外，化合物4b可以影响生物膜的形成，抑制细胞外多糖的产生，最终降低Xoo的致病性。所有结果表明，带有酰腙和苯并噻唑部分的双亚砜衍生物可用于开发具有高抗菌活性的小分子农药。