Synthesis and Insecticidal Activity Evaluation of Potential Insecticidal Natural Product Borrelidin Analogs Toward New Pesticides

Abstract

Moth pests are at particularly high risk of acquiring insecticide resistance among agricultural pests. Therefore, pesticide seeds with novel mechanisms of action that are effective in controlling moth pests are in demand. In our previous study, we identified borrelidin (1) as a promising pesticide candidate with a new mechanism of action. However, borrelidin analogs with insecticidal activity had not been synthesized and evaluated. In this study, we synthesized 19 derivatives from 1 and evaluated their insecticidal activity against first instar larvae of silkworms and common cutworms (Spodoptera litura, CCW). Our investigation facilitated to reveal the detailed structure–activity relationships and discover a novel derivative showing effectiveness against the moth pests.