A Potential Lead for Insect Growth Regulator: Design, Synthesis, and Biological Activity Evaluation of Novel Hexacyclic Pyrazolamide Derivatives

文献类型： 外文期刊

第一作者： Guo, Bingbo

作者： Guo, Bingbo;Jiang, Biaobiao;Jin, Xiaoyu;Wang, Liuyang;Yang, Zhaokai;Luo, Shihui;Zhang, Li;Yang, Xinling;Wang, Chunying;Yang, Qing

作者机构：

关键词： insect growth regulators; pyrazolamide; ecdysone receptor; chitinase; molecular docking; dual-target IGRs

期刊名称：MOLECULES （ 影响因子：4.6； 五年影响因子：4.9 ）

ISSN：

年卷期： 2023 年 28 卷 9 期

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收录情况： SCI

摘要： Ecdysone receptor (EcR) and chitinase play a critical role in the molting stage of insect pests. Each of them is considered a promising target for the development of novel insect growth regulators (IGRs). In the present paper, a total of 24 (23 novel) hexacyclic pyrazolamide derivatives were designed and synthesized by reducing the heptacycle and inserting small flexible linkers on the basis of the previously discovered dual-target compound D-27 acting simultaneously on EcR and Ostrinia furnacalis chitinase (OfChtI). Their insecticidal activities against Plutella xylostella, Spodoptera frugiperda, and Ostrinia furnacalis larvae were evaluated. The results revealed that the insecticidal activity was not significantly enhanced when the heptacycle on the pyrazole ring was reduced to a hexacycle. However, the insertion of an additional methylene spacer between the substituted phenyl ring and the amide bond can improve the insecticidal activity. Among the derivatives, the most potent compound, 6j, exhibited promising insecticidal activities against P. xylostella and S. frugiperda. Further protein binding assays and molecular docking indicated that 6j could target both EcR and OfChtI, and is a potential lead compound for IGRs. The present work provides valuable clues for the development of new dual-target IGRs.

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