Design, Synthesis, and Insecticidal Activities of Novel N-pyridylpyrazole Amide Derivatives Containing a Maleimide.

Abstract

To discover "me-better" insecticidal active molecules targeting ryanodine receptors (RyRs), a series of novel N-pyridylpyrazole amide derivatives containing a maleimide were designed and synthesized in accordance with the prior investigations of our group. Preliminary bioassay findings indicated some compounds containing a maleimide exhibited good larvicidal activities against lepidopteran pests at a concentration of 500 mg L-1. Compound 9j showed 60% larvicidal activities against M. Separata at 50 mg L-1. Compound 9b exhibited 40% larvicidal activities against P. xylostella at 50 mg L-1. Molecular docking study indicated that H-bonds, π-π interaction and cation-π interaction made for the binding of compounds 9b, 9j with P. Xylostella RyR. These results indicated that compounds 9b and 9j could be developed as novel and promising insecticidal leads.