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双(吲哚基)-酰肼-腙衍生物的设计与合成及其对植物病原真菌的抗真菌活性

Design and synthesis of bis(indolyl)-hydrazide-hydrazone derivatives and their antifungal activities against plant pathogen fungi.

作者信息

Huang Haowei, Tang Jinrui, Dang Kunrong, Tang Jiayue, Li Enxian, Fan Liming, Ye Min, Wu Guoxing, Su Fawu

机构信息

State Key Laboratory for Conservation and Utilization of Bio-Resources in Yunnan, School of Plant Protection, Yunnan Agricultural University, Kunming, China.

出版信息

Nat Prod Res. 2024 Jun 28:1-6. doi: 10.1080/14786419.2024.2371994.

DOI:10.1080/14786419.2024.2371994
PMID:38940256
Abstract

A series of bis(indolyl)-hydrazide-hydrazone derivatives were synthesised, and their structures were characterised using H-NMR and HRMS. The antifungal activity of the prepared compounds was evaluated against Cav., Penz., Pers.: Fr. and Kühn using the mycelial growth rate method. The preliminary bioassays revealed that most of the synthesised compounds exhibited antifungal activity against the four tested fungi and displayed a remarkable inhibitory effect on the mycelium growth of . In particular, compounds 3b, 3c, and 3k demonstrated significant antifungal activity against , with EC values of 26.42, 20.74, and 22.41 μM, respectively, outperforming the positive control shenqinmycin (47.18 μM) and carvacrol (49.13 μM).

摘要

合成了一系列双(吲哚基)-酰肼腙衍生物,并使用氢核磁共振(H-NMR)和高分辨质谱(HRMS)对其结构进行了表征。采用菌丝生长速率法,对所制备化合物针对辣椒疫霉(Phytophthora capsici Leonian)、稻瘟病菌(Magnaporthe oryzae (T.T. Hebert) Barr)、核盘菌(Sclerotinia sclerotiorum (Lib.) de Bary)和禾谷镰刀菌(Fusarium graminearum Schwabe)的抗真菌活性进行了评估。初步生物测定表明,大多数合成化合物对四种受试真菌均表现出抗真菌活性,并对稻瘟病菌的菌丝生长显示出显著的抑制作用。特别是,化合物3b、3c和3k对稻瘟病菌表现出显著的抗真菌活性,其半数效应浓度(EC)值分别为26.42、20.74和22.41μM,优于阳性对照申嗪霉素(47.18μM)和香芹酚(49.13μM)。

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