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Synthesis and antiviral activity of novel myricetin derivatives containing ferulic acid amide scaffolds
New Journal of Chemistry ( IF 3.3 ) Pub Date : 2020/01/10 , DOI: 10.1039/c9nj05867b
Xu Tang 1, 2, 3, 4, 5 , Cheng Zhang 1, 2, 3, 4, 5 , Mei Chen 1, 2, 3, 4, 5 , Yining Xue 6, 7, 8, 9, 10 , Tingting Liu 1, 2, 3, 4, 5 , Wei Xue 1, 2, 3, 4, 5
Affiliation  

A variety of myricetin derivatives bearing ferulic acid amide scaffolds were designed and synthesized. The structures of all title compounds were determined by 1H NMR, 13C NMR, 19F NMR and HRMS. Preliminary bioassays suggested that some of the target compounds exhibited remarkable antiviral activities. In particular, compound 4l possessed significant protective activity against tobacco mosaic virus (TMV), with a half maximal effective concentration (EC50) value of 196.11 μg mL−1, which was better than that of commercial agent ningnanmycin (447.92 μg mL−1). Meanwhile, microscale thermophoresis (MST) indicated that compound 4l has strong binding capability to the tobacco mosaic virus coat protein (TMV-CP) with a dissociation constant (Kd) value of 0.34 μmol L−1, which was better than that of ningnanmycin (0.52 μmol L−1). These results suggested that novel myricetin derivatives bearing ferulic acid amide scaffolds may be considered as an activator for antiviral agents.

中文翻译:

含阿魏酸酰胺支架的新型杨梅素衍生物的合成及抗病毒活性

设计并合成了多种带有阿魏酸酰胺支架的杨梅素衍生物。所有标题化合物的结构通过1 H NMR,13 C NMR,19 F NMR和HRMS确定。初步的生物测定表明,某些目标化合物表现出显着的抗病毒活性。尤其是,化合物4l对烟草花叶病毒(TMV)具有明显的保护活性,最大有效浓度(EC 50)值的一半为196.11μgmL -1,优于商业制剂宁南霉素(447.92μgmL -1)。)。同时,微型热泳(MST)表明化合物4l具有与烟草花叶病毒外壳蛋白(TMV-CP)的强结合能力,解离常数(K d)值为0.34μmolL -1,优于宁南霉素的解离常数(0.52μmolL -1)。这些结果表明,带有阿魏酸酰胺支架的新型杨梅素衍生物可以被认为是抗病毒剂的活化剂。
更新日期:2020-02-12
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