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首页> 外文期刊>RSC Advances >Synthesis and antibacterial and antiviral activities of myricetin derivatives containing a 1,2,4-triazole Schiff base
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Synthesis and antibacterial and antiviral activities of myricetin derivatives containing a 1,2,4-triazole Schiff base

机译：含1,2,4-三唑希夫碱的杨梅素衍生物的合成及其抗菌和抗病毒活性

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A series of novel myricetin derivatives containing a 1,2,4-triazole Schiff base were designed and synthesized. Their structures were systematically characterized using ~(1) H NMR, ~(13) C NMR, and HRMS. During antibacterial bioassays, 6f , 6i , and 6q demonstrated a good inhibitory effect against Xanthomonas axonopodis pv. citri ( Xac ), with half-maximal effective concentration (EC _(50) ) values of 10.0, 9.4, and 8.8 μg mL ~(?1) , respectively, which were better than those of bismerthiazol (54.9 μg mL ~(?1) ) and thiodiazole copper (61.1 μg mL ~(?1) ). Note that 6w demonstrated a good inhibitory effect against Ralstonia solanacearum ( Rs ) with and EC _(50) value of 15.5 μg mL ~(?1) , which was better than those of bismerthiazol (55.2 μg mL ~(?1) ) and thiodiazole copper (127.9 μg mL ~(?1) ). Similarly, 6a , 6d , and 6e demonstrated a good inhibitory effect against Xanthomonas oryzae pv. oryzae ( Xoo ) with EC _(50) values of 47.1, 61.2, and 61.0 μg mL ~(?1) , respectively, which were better than those of bismerthiazol (148.2 μg mL ~(?1) ) and thiodiazole copper (175.5 μg mL ~(?1) ). Furthermore, we used scanning electron microscopy (SEM) to study the possible sterilization process of the target compound 6q against Xac . The results indicated the possibility of destroying the bacterial cell membrane structure, resulting in an incomplete bacterial structure, and thus achieving inhibition. Furthermore, antiviral bioassays revealed that most compounds exhibited excellent antiviral activity against tobacco mosaic virus (TMV) at a concentration of 500 μg mL ~(?1) . The results of the molecular docking studies for 6g with TMV-CP (PDB code: 1EI7) showed that compound 6g had partially interacted with TMV-CP. Therefore, mechanistic studies of the action of compound 6g could be further studied based on that.
机译：设计并合成了一系列含有1,2,4-三唑希夫碱的新型杨梅素衍生物。使用〜（1）H NMR，〜（13）C NMR和HRMS系统地表征了它们的结构。在抗菌生物测定过程中，6f，6i和6q表现出对轴突黄单胞菌pv的良好抑制作用。柠檬酸（Xac）的半数最大有效浓度（EC _（50））值分别为10.0、9.4和8.8μgmL〜（？1），比比美噻唑（54.9μgmL〜（？） 1））和硫代二唑铜（61.1μgmL〜（？1））。注意6w表现出对青枯雷尔氏菌（Rsstonia solanacearum，Rs）的良好抑制作用，其EC_（50）值为15.5μgmL〜（？1），优于比美沙唑（55.2μgmL〜（？1））和硫代二唑铜（127.9μgmL〜（？1））。同样，6a，6d和6e表现出对米黄单胞菌pv的良好抑制作用。米曲霉（Xoo）的EC _（50）值分别为47.1、61.2和61.0μgmL〜（？1），分别优于比美噻唑（148.2μgmL〜（？1））和硫二唑铜（175.5）微克mL〜（？1））。此外，我们使用扫描电子显微镜（SEM）研究了目标化合物6q对Xac的可能灭菌过程。结果表明可能破坏细菌细胞膜结构，导致不完整的细菌结构，从而达到抑制作用。此外，抗病毒生物测定法显示，大多数化合物在500μgmL〜（？1）的浓度下对烟草花叶病毒（TMV）表现出优异的抗病毒活性。用TMV-CP（PDB代码：1EI7）对6g进行分子对接研究的结果表明，化合物6g与TMV-CP部分相互作用。因此，可以据此进一步研究化合物6g的作用机理。

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