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Synthesis and antibacterial activity of chalcone derivatives containing thioether triazole
Journal of Heterocyclic Chemistry ( IF 2.4 ) Pub Date : 2020-01-09 , DOI: 10.1002/jhet.3755
Ying Chen 1 , Pu Li 1 , Mei Chen 1 , Jun He 1 , Shijun Su 1 , Ming He 1 , Hua Wang 2 , Wei Xue 1
Affiliation  

The infection of Xanthomonas oryzae pv. Oryzae (Xoo), Ralstonia solanacearum (Rs), and Xanthomonas axonopodis pv. Citri (Xac) has become a major problem in agricultural production. In this study, a series of novel chalcone derivatives containing thioether triazoles were designed and synthesized. The structures of the novel compounds were systematically characterized via 1H‐NMR, 13C‐NMR, and HRMS. Moreover, the antibacterial activity results showed that E10, E11, E15, and E16 have adequate antibacterial activities against Xoo, Rs, and Xac. Among the different compounds, E15 exhibited remarkable inhibitory effect against Xac with an EC50 of 9.1 μg.mL‐1, which was better than that of commercial agent bismerthiazol (54.9 μg.mL‐1). In addition, the possible antibacterial mechanism of the target compound E15 against Xac was studied via scanning electron microscopy (SEM).

中文翻译:

含硫醚三唑查尔酮衍生物的合成及抑菌活性

米糠黄单胞菌的感染。OryzaeXoo),Ralstonia solanacearumRs)和Xanthomonas axonopodis pv。柠檬Xac)已成为农业生产中的主要问题。在这项研究中,设计并合成了一系列新型的含硫醚三唑的查尔酮衍生物。通过 1 H-NMR,13 C-NMR和HRMS系统地表征了新型化合物的结构。此外,抗菌活性结果表明,E 10,E 11,E 15和E 16XooRsXac具有足够的抗菌活性。在不同的化合物中,E 15Xac表现出显着的抑制作用,EC 50为9.1μg.mL -1,比商品试剂比美噻唑(54.9μg.mL -1)更好。另外,通过扫描电子显微镜(SEM)研究了目标化合物E 15Xac的可能的抗菌机理。
更新日期:2020-01-09
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