Junia, Health and Environment, Laboratory of Sustainable Chemistry and Health, F-59000, Lille, France.
Sorbonne University, Université de technologie de Compiègne, ESCOM, EA TIMR 4297, Centre de recherche de Royallieu, CS 60319, 60203, Compiègne cedex, France.
Chem Biodivers. 2021 Nov;18(11):e2100224. doi: 10.1002/cbdv.202100224. Epub 2021 Sep 28.
As new environmentally friendly and effective antifungal agents are deeply needed, efficient ecofriendly strategies were designed to access two series of compounds inspired from natural γ-lactams. Designed compounds were fully characterized and evaluated as antifungal candidates against Zymoseptoria tritici, the main pathogen on wheat crops. The targeted derivatives were prepared from natural resources using green solvents, simple procedures, and limited purification steps. These bio-inspired compounds revealed as good candidates for further development of efficient crop protection products. Indeed, the HIT compounds exhibited IC around 1 μg/mL and were more active than the references tebuconazole and bixafen towards some multidrug-resistant strains. Two dozen of derivatives have been obtained for each series and allowed to establish early structure-activity relationships useful for the development of next generation of γ-lactam derivatives with improved efficacy.
由于迫切需要新型环保且有效的抗真菌剂，因此设计了高效环保的策略来获得受天然 γ-内酰胺启发的两个系列的化合物。设计的化合物进行了全面的表征，并作为抗小麦作物上的主要病原体——小麦基腐病菌的候选抗真菌剂进行了评估。目标衍生物采用绿色溶剂、简单的程序和有限的纯化步骤从天然资源中制备。这些受生物启发的化合物有望进一步开发高效的作物保护产品。事实上，HIT 化合物的 IC 值约为 1μg/mL，并且对一些多药耐药菌株的活性比对照药剂咯菌腈和双炔酰菌胺更强。每个系列都获得了二十几种衍生物，这为开发具有增效作用的新一代 γ-内酰胺衍生物建立了早期的结构-活性关系。
