Synthesis and Biological Evaluation of Benzimidazole Phenylhydrazone Derivatives as Antifungal Agents against Phytopathogenic Fungi.

Synthesis and Biological Evaluation of Benzimidazole Phenylhydrazone Derivatives as Antifungal Agents against Phytopathogenic Fungi.
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苯并咪唑苯腙衍生物抗植物病原真菌的合成及生物学评价

DOI:
10.3390/molecules21111574
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发表时间:
2016-11-22
期刊:
Molecules (Basel, Switzerland)
影响因子:
--
通讯作者:
Ye YH
Ye YH
中科院分区:
其他
文献类型:
--
作者:
Wang X;Chen YF;Yan W;Cao LL;Ye YH

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合成了一系列苯并咪唑苯腙衍生物(6a-6ai),并通过1H-NMR、ESI-MS和元素分析对其结构进行了表征。通过单晶X射线衍射进一步证实了6 b的结构为(E)-构型。采用菌丝生长速率法对所有化合物进行了抗立枯丝核菌和稻瘟病菌的活性筛选。化合物6 f显示出明显的抗红曲霉活性。solani和M. EC_(50)分别为1.20和1.85 μg/mL。活体试验表明,6 f能有效地防治由上述两种病原菌引起的水稻纹枯病和稻瘟病。本工作表明,具有苯并咪唑苯腙骨架的化合物6 f可以被认为是开发新型杀菌剂的先导结构。
A series of benzimidazole phenylhydrazone derivatives (6a–6ai) were synthesized and characterized by 1H-NMR, ESI-MS, and elemental analysis. The structure of 6b was further confirmed by single crystal X-ray diffraction as (E)-configuration. All the compounds were screened for antifungal activity against Rhizoctonia solani and Magnaporthe oryzae employing a mycelium growth rate method. Compound 6f exhibited significant inhibitory activity against R. solani and M. oryzae with the EC50 values of 1.20 and 1.85 μg/mL, respectively. In vivo testing demonstrated that 6f could effectively control the development of rice sheath blight (RSB) and rice blast (RB) caused by the above two phytopathogens. This work indicated that the compound 6f with a benzimidazole phenylhydrazone scaffold could be considered as a leading structure for the development of novel fungicides.
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