Pest management science · 2026
Revolutionizing anti-fungal strategies: novel Chromone-based microtubulin target fungicides for Sclerotinia Sclerotiorum of oilseed rape.
СтатьяНазвание и аннотация: Перевод в очереди
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Shao Lihui, Wu Ying, Hu Xianqun, Zhang Bo, Zhou Xiang, Yang Song
Аннотация
BACKGROUND: Addressing escalating pesticide resistance and food security necessitates sustainable plant pathogen management. This study rationally designed and synthesized novel chromone-acylhydrazone derivatives engineered to target fungal tubulin, aiming to provide new avenues for disease control.
RESULTS: We successfully designed and synthesized a series of novel chromone-acylhydrazone derivatives. Compound H9 emerged as a highly potent lead, exhibiting remarkable inhibitory activity against Sclerotinia sclerotiorum with an EC50 of 0.23 μg mL-1. Mechanistic studies revealed that H9's 3-fluorobenzoylhydrazide moiety disrupts microtubule polymerization via critical hydrogen bonding, while the chromone core facilitates favorable π-alkyl interactions. H9 demonstrated promising pharmacokinetic profiles and negligible mammalian toxicity. Further, encapsulation within polyurethane microcapsules (H9-Loaded PU MCs) yielded an efficient (89.12% encapsulation efficiency) sustained-release system, significantly improving foliar adhesion and fungicidal efficacy.
CONCLUSIONS: This work highlights H9 as a groundbreaking, safe fungicide, whose exceptional bioactivity, favorable safety profile, and advanced sustained-release formulation technology offer a powerful solution for next-generation sustainable pest management. This underscores the significant potential of rational molecular design coupled with advanced formulation technology in advancing pesticide candidates with green potential. © 2026 Society of Chemical Industry.
RESULTS: We successfully designed and synthesized a series of novel chromone-acylhydrazone derivatives. Compound H9 emerged as a highly potent lead, exhibiting remarkable inhibitory activity against Sclerotinia sclerotiorum with an EC50 of 0.23 μg mL-1. Mechanistic studies revealed that H9's 3-fluorobenzoylhydrazide moiety disrupts microtubule polymerization via critical hydrogen bonding, while the chromone core facilitates favorable π-alkyl interactions. H9 demonstrated promising pharmacokinetic profiles and negligible mammalian toxicity. Further, encapsulation within polyurethane microcapsules (H9-Loaded PU MCs) yielded an efficient (89.12% encapsulation efficiency) sustained-release system, significantly improving foliar adhesion and fungicidal efficacy.
CONCLUSIONS: This work highlights H9 as a groundbreaking, safe fungicide, whose exceptional bioactivity, favorable safety profile, and advanced sustained-release formulation technology offer a powerful solution for next-generation sustainable pest management. This underscores the significant potential of rational molecular design coupled with advanced formulation technology in advancing pesticide candidates with green potential. © 2026 Society of Chemical Industry.