State Key Laboratory of Green Pesticide, Center for R&D of Fine Chemicals, Guizhou University, Guiyang 550025, P. R. China.
J Agric Food Chem. 2024 Nov 13;72(45):25034-25044. doi: 10.1021/acs.jafc.4c08663. Epub 2024 Nov 5.
A series of myricetin derivatives containing diisopropanolamine were designed and synthesized. The in vitro inhibitory effects of the target compounds on 9 fungal pathogens and 3 bacterial pathogens were also evaluated. had the best inhibitory effect against (), with an EC value of 4.9 μg/mL, which was better than zinc-thiazole (ZT: EC = 7.3 μg/mL) and thiodiazole-copper (TC: EC = 65.5 μg/mL); had the best inhibitory effect against . (), with an EC value of 17.2 μg/mL, which was better than azoxystrobin (Az: EC = 22.3 μg/mL). In vivo inhibition tests were performed on kiwifruit for and rice leaves for . At 200 μg/mL, the curative activity of against rice leaf blight was 40.7%, which was better than that of ZT (37.2%) and TC (32.9%), and the protective activity of was 44.8%, which was better than that of ZT (39.5%) and TC (34.6%). The curative activity of against kiwi soft rot disease was 70.1%, which was better than that of Az (62.8%). Preliminary elucidation of the possible mechanisms of action was carried out by experiments on fluorescence microscopy, scanning electron microscopy, formation of biofilms, density functional theory calculations, and so on.
设计并合成了一系列含有二异丙醇胺的杨梅素衍生物。还评估了目标化合物对 9 种真菌病原体和 3 种细菌病原体的体外抑制作用。
对 （）抑制效果最好，EC 值为 4.9 μg/mL，优于锌噻唑（ZT：EC = 7.3 μg/mL）和噻二唑铜（TC：EC = 65.5 μg/mL）；对 （）抑制效果最好，EC 值为 17.2 μg/mL，优于肟醚菌胺（Az：EC = 22.3 μg/mL）。在猕猴桃上进行了活体抑制试验，在水稻叶片上进行了 。在 200 μg/mL 时，化合物 对水稻稻瘟病的治疗活性为 40.7%，优于 ZT（37.2%）和 TC（32.9%），保护活性为 44.8%，优于 ZT（39.5%）和 TC（34.6%）。化合物 对猕猴桃软腐病的治疗活性为 70.1%，优于肟醚菌胺（Az：62.8%）。通过荧光显微镜、扫描电子显微镜、生物膜形成、密度泛函理论计算等实验初步阐明了可能的作用机制。
