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 9 j showed 60 % larvicidal activities against M. Separata at 50 mg L^-1 . Compound 9 b 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 9 b, 9 j with P. Xylostella RyR. These results indicated that compounds 9 b and 9 j could be developed as novel and promising insecticidal leads.

Keywords: larvicidal activities; maleimide; molecular docking; ryanodine receptors.