AUTHOR=Zhang Chiying , Tian Qingqiang , Li Yahui 

TITLE=Design, synthesis, and insecticidal activity evaluation of piperine derivatives

JOURNAL=Frontiers in Chemistry

VOLUME=10

YEAR=2022

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2022.973630

DOI=10.3389/fchem.2022.973630

ISSN=2296-2646

ABSTRACT=<p>Structural optimization of natural products has become one of the most effective ways to develop novel pesticides. In this study, 30 novel pesticide derivatives containing a linear bisamide were synthesized. Then, their insecticidal activities against <italic>P. xylostella</italic> were evaluated. Results indicate that different bisamide substitutes show different larvicidal structure–activity relationships. At the same time, 2-trifluoroethyl is the most efficient substituent. The bioactivity results showed that most of the desired compounds exhibited better insecticidal activity against <italic>P. xylostella</italic> than piperine. Among them, <bold>compound D28</bold> resulted in 90% mortality at 1 mg/ml concentration. This study provides a novel protocol for the discovery of new insecticides. The molecular docking results indicated that compound D28 could act on <italic>γ</italic>-aminobutyric acid receptors.</p>