Discovery of Potent N-Methylcarbamoylguanidino Insect Growth Regulators Targeting OfChtI and OfChi-h

文献类型： 外文期刊

第一作者： Zhao, Zhixiang

作者： Zhao, Zhixiang;Dong, Yanhong;Lu, Huizhe;Zhang, Jianjun;Chen, Wei;Yang, Qing;Yang, Qing

作者机构：

关键词： Chitinase; OfChtI; OfChi-h; inhibitor; N-methylcarbamoylguanidino; insecticides

期刊名称：JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY （ 影响因子：6.1； 五年影响因子：6.3 ）

ISSN： 0021-8561

年卷期： 2023 年

页码：

收录情况： SCI

摘要： Insect growth regulators (IGRs) are important insecticidesthatreduce the harm caused by insects to crops by controlling pest populationgrowth. Chitinases are closely associated with insect growth and areamong the most important glycoside hydrolases. Thus, Chitinase isan attractive target for the development of novel insecticides. Inthis study, we designed and synthesized a series of novel and highlypotent insecticides targeting OfChtI and OfChi-h in insects. Enzymatic activity tests showed thatmost compounds exhibited a potent inhibitory activity against OfCh-h. Binding mode analysis revealed that the target compoundsbound to the -1 active subsite of Chitinase through the keypharmacophore N-methylcarbamoylguanidino. Compounds 6e, 6g, 6j, and 6o significantlyaffected the growth and development of Plutella xylostella at 200 mg/L. Our study provides novel insights for the developmentof potent insecticide-targeted Chitinase combinations based on receptorsand ligands.

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