Abstract:
To discover novel phenylpyrazole acaricides/insecticides with enhanced activity and structural diversity, a series of 14 nicofluprole derivatives were designed and synthesized through pharmacophore fusion strategy using nicofluprole as the lead compound. The structures of target compounds were confirmed by
1H NMR,
13C NMR, and HRMS. Acaricidal/insecticidal activities against
Tetranychus cinnabarinus,
Plutella xylostella, and
Mythimna separata were systematically evaluated. Bioassay results revealed that several compounds exhibited over 85% mortality against
T. cinnabarinus at a concentration of 4 mg/L. Notably, compounds
7a and
7b demonstrated superior acaricidal activities of 93.7% and 89.5% respectively, showing significant improvement compared to the parent compound nicofluprole. These compounds could serve as promising lead candidates for further investigation. Additionally, the preliminary structure-activity relationship analysis based on the bioassay data provided theoretical guidance for subsequent research and development of related acaricides/insecticides.