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Molecules 2016, 21(11), 1574;

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

State & Local Joint Engineering Research Center of Green Pesticide Invention and Application, College of Plant Protection, Nanjing Agricultural University, Nanjing 210095, China
Key Laboratory of Integrated Management of Crop Diseases and Pests, Ministry of Education, Nanjing 210095, China
These authors contributed equally to this paper.
Author to whom correspondence should be addressed.
Academic Editors: Daniela Barlocco and Fiorella Meneghetti
Received: 13 October 2016 / Revised: 8 November 2016 / Accepted: 12 November 2016 / Published: 22 November 2016
(This article belongs to the Special Issue Frontiers in Antimicrobial Drug Discovery and Design)
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A series of benzimidazole phenylhydrazone derivatives (6a6ai) 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. View Full-Text
Keywords: benzimidazole; phenylhydrazone; antifungal activity benzimidazole; phenylhydrazone; antifungal activity

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Wang, X.; Chen, Y.-F.; Yan, W.; Cao, L.-L.; Ye, Y.-H. Synthesis and Biological Evaluation of Benzimidazole Phenylhydrazone Derivatives as Antifungal Agents against Phytopathogenic Fungi. Molecules 2016, 21, 1574.

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