Insect growth regulators (IGRs), which can interrupt or inhibit pest life cycles, are low-toxicity pesticides widely used in integrated pest management (IPM). Ecdysone analogues and chitinase inhibitors are familiar IGRs that have attracted considerable attention because of their unique modes of action and low toxicity to non-target organisms. To find new and highly effective candidate IGRs with novel mechanisms, D-08 (N-(4-(tert-butyl)phenyl)-2-phenyl-2,4,5,6,7,8-hexahydrocyclohepta[c]pyrazole-5-carboxamide) was chosen as a lead compound, and a series of novel heptacyclic pyrazolamide derivatives were designed and synthesized using the scaffold hopping strategy. The bioassay showed that III-27 (N-(2-methylphenethyl)-1-phenyl-1,4,5,6,7,8-hexahydrocyclohepta[c]pyrazole-5-carboxamide) had excellent activity against Plutella xylostella. Protein verification and molecular docking indicated that III-27 could act on both the ecdysone receptor (EcR) and Ostrinia furnacalis chitinase (Of ChtI) and is a promising new lead IGRs. The interaction mechanism of III-27 with EcR and Of ChtI was then studied by molecular docking. These results provide important guidance for the study of new dual-target IGRs.

昆虫生长调节剂（IGR）可以中断或抑制有害生物的生命周期，是广泛用于有害生物综合治理（IPM）的低毒农药。蜕皮激素类似物和几丁质酶抑制剂是众所周知的IGR，因其独特的作用方式和对非靶标生物的低毒性而备受关注。为了找到具有新颖机理的新型高效候选IGR，D-08（N-（4-（叔丁基）苯基）-2-苯基-2,4,5,6,7,8-六氢环庚基[ c ]吡唑选择了-5-甲酰胺作为前导化合物，并使用支架跳跃策略设计并合成了一系列新型的七环吡唑酰胺衍生物。生物测定表明，III-27（N-（2-甲基苯乙基）-1-苯基-1,4,5,6,7,8-六氢环庚[ c ]吡唑-5-羧酰胺）对小菜蛾具有优异的活性。蛋白质验证和分子对接表明，III-27可以同时在蜕皮激素受体（ECR）和行为玉米螟几丁质酶（中ChtI），是一个有前途的新铅闪联。的相互作用机制III-27与的EcR和中ChtI然后通过分子对接研究。这些结果为研究新型双靶IGRs提供了重要的指导。