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Synthesis and biological evaluation of 2-(4-substituted benzene-1-sulfonyl)- N' -(substituted-1-sulfonyl)acetohydrazide as antibacterial agents
Chemical Papers ( IF 2.1 ) Pub Date : 2020-07-06 , DOI: 10.1007/s11696-020-01271-6
Pei Li , Junliang Zhou , Yan Liu , Xiang Wang

In this study, a series of new sulfone derivatives containing a sulfonohydrazide moiety were synthesized and their structures were determined using 1H NMR, 13C NMR, and HRMS. Then, the in vitro antibacterial activities against Xanthomonas oryzae pv. oryzae (Xoo) and Xanthomonas axonopodis pv. citri (Xac) were evaluated by performing turbidimeter test. Bioactivity results showed that compound 2-(4-fluorobenzene-1-sulfonyl)-N′-(4-fluorobenzene-1-sulfonyl)acetohydrazide (5g) revealed the best antibacterial activities against Xoo and Xac, with the 50% effective concentration (EC50) values of 25 and 36 µg/mL, respectively, which were superior to those of thiodiazole copper (110 and 230 µg/mL, respectively) and bismerthiazol (84 and 146 µg/mL, respectively).



中文翻译:

2-(4-取代苯-1-磺酰基)-N'-(取代-1-磺酰基)乙酰肼作为抗菌剂的合成及生物学评价

在这项研究中,合成了一系列含有磺酰肼部分的新砜衍生物,并使用1 H NMR,13 C NMR和HRMS确定了它们的结构。然后,体外对米黄单胞菌PV的抗菌活性。Xoo)和黄单胞菌xanthomonas axonopodis pv。通过进行浊度计测试评价柠檬酸Xac)。生物活性结果表明,化合物2-(4-氟苯-1-磺酰基)-N' -(4-氟苯-1-磺酰基)乙酰肼(5g)对XooXac具有最佳的抗菌活性。,其50%有效浓度(EC 50)值分别为25和36 µg / mL,优于硫代二唑铜(分别为110和230 µg / mL)和比美噻唑(84和146 µg / mL),分别)。

更新日期:2020-09-12
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