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Design, synthesis and bioactivity evaluation of novel thioether derivatives containing a sulfonohydrazide moiety
Phosphorus, Sulfur, and Silicon and the Related Elements ( IF 1.4 ) Pub Date : 2020-06-05 , DOI: 10.1080/10426507.2020.1762194
Pei Li 1 , Junliang Zhou 2 , Yan Liu 3 , Xiang Wang 1
Affiliation  

Abstract A series of novel thioether derivatives containing a sulfonohydrazide moiety were synthesized and determined using 1H NMR, 13C NMR, HRMS, and elemental analysis. Their in vitro antibacterial activities against Xanthomonas oryzae pv. oryzae (Xoo) and Xanthomonas axonopodis pv. citri (Xac) were investigated by performing turbidimeter test. Bioassay results showed that some of the target compounds revealed moderate to good antibacterial activities against Xoo and Xac. Especially, N’-(2-(ethylthio)acetyl)-4-fluorobenzenesulfonohydrazide (4p) revealed the best bioactivities against Xoo and Xac, with the 50% effective concentration (EC50) values of 13.75 and 18.56 μg/mL, respectively, which were even better than those of thiodiazole copper and bismerthiazol. Graphical Abstract

中文翻译:

含有磺酰肼部分的新型硫醚衍生物的设计、合成和生物活性评估

摘要 合成了一系列含有磺酰肼部分的新型硫醚衍生物,并使用 1H NMR、13C NMR、HRMS 和元素分析进行​​了测定。它们对 Xanthomonas oryzae pv 的体外抗菌活性。oryzae (Xoo) 和 Xanthomonas axonopodis pv。通过进行浊度计测试来研究柑橘 (Xac)。生物测定结果表明,一些目标化合物对 Xoo 和 Xac 显示出中等至良好的抗菌活性。特别是,N'-(2-(乙硫基)乙酰基)-4-氟苯磺酰肼 (4p) 显示出对 Xoo 和 Xac 的最佳生物活性,50% 有效浓度 (EC50) 值分别为 13.75 和 18.56 μg/mL,甚至优于噻二唑铜和双甲噻唑。图形概要
更新日期:2020-06-05
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