Recent advances in isoxazoline and isoxazole scaffolds as insecticidal agents: synthesis, and activity

The increasing resistance of insect pests to conventional insecticides has heightened the urgency to discover novel chemical scaffolds that offer enhanced efficacy, selectivity, and safety profiles. Among these, isoxazoline analogs have recently emerged as a promising class of urban insecticides, demonstrating broad-spectrum activity against various agricultural and urban pests. This review aims to provide a thorough overview of advancements in the synthesis, structural diversity, and insecticidal applications of isoxazolines and isoazoles from 2016 to 2026. Recent progress in synthetic methodologies, including green chemistry approaches and innovative catalytic systems, has facilitated efficient and sustainable access to diverse isoxazoline frameworks. Structure-activity relationship studies have identified key modifications that improve insecticidal potency and selectivity while emphasizing the possibility of hybrid molecules to counteract resistance mechanisms. In addition to their high efficacy, isoxazoline- and isoxazole-based insecticides generally show favorable toxicological and environmental profiles, posing reduced risks to humans and non-target organisms compared to many traditional insecticides. The review further discusses the mechanisms of action of isoxazolines, their incorporation into integrated pest management (IPM) strategies, and their commercial applications in urban and agricultural pest control. Lastly, it addresses current challenges and future research directions, underscoring the necessity for ongoing innovation and safety assessments to ensure the sustainable use of isoxazolines and isoxazoles in modern agriculture.