Design, synthesis, biologically evaluation and molecular docking of C-glycosidic oximino carbamates as novel OfHex1 inhibitors

文献类型： 外文期刊

第一作者： Liang, Peibo

作者： Liang, Peibo;Xu, Qingbo;Chen, Ruizhe;Jin, Shuhui;Zhang, Jianjun;Yang, Qing;He, Danchan;Yang, Qing;He, Danchan;Yang, Qing

作者机构：

关键词： C-Glycosides; beta-N-acetyl-D-hexosaminidase; OfHex1; Enzyme inhibitors; Molecular docking; Larvicidal activity

期刊名称：CARBOHYDRATE RESEARCH （ 影响因子：2.975； 五年影响因子：2.535 ）

ISSN： 0008-6215

年卷期： 2022 年 520 卷

页码：

收录情况： SCI

摘要： The inhibition of function-specific beta-N-acetyl-D-hexosaminidases, such as OfHex1 from the Asian corn borer (Ostrinia furnacalis), is a promising strategy for the development of green pesticides. Among reported OfHex1 inhibitors, glycosyl inhibitors show especially high inhibitory activity. In this study, a series of novel C-glycosidic oximino carbamate derivatives were designed using the OfHex1 crystal structure and synthesized. Among the C -Glycoside derivatives studied, compound 7k exhibited the best inhibitory activity against OfHex1 (IC50 = 47.47 mu M). Compound 7k also exhibited excellent larvicidal activity against Plutella xylostella. The potential inhibitory mechanism of 7k was studied using molecular docking. Notably, compound 7k is the first reported C-glycoside inhibitor of OfHex1. These results provide direction for the rational design of novel OfHex1 inhibitors.

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