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Molecules 2017, 22(12), 2085;

Design, Synthesis, and Fungicidal Activity of Novel Thiosemicarbazide Derivatives Containing Piperidine Fragments

Department of Applied Chemistry, College of Science, China Agricultural University, Beijing 100193, China
Author to whom correspondence should be addressed.
Received: 6 November 2017 / Revised: 23 November 2017 / Accepted: 27 November 2017 / Published: 11 December 2017
(This article belongs to the Special Issue Emerging Drug Discovery Approaches against Infectious Diseases)
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In order to discover novel eco-friendly lead compounds for plant pathogenic fungi control, a series of benzaldehyde thiosemicarbazide derivatives with a piperidine moiety have been designed and synthesized. Fungicidal activities of all the synthesized compounds were evaluated in vitro. The results indicated that all the title compounds exhibited moderate to good fungicidal activities. Compound 3b displayed excellent activities against Pythium aphanidermatum, Rhizoctonia solani, Valsa mali, and Gaeu-mannomyces graminsis, with EC50 values lower than 10 μg/mL. Especially, in the case of Pythium aphanidermatum, its activity (EC50 = 1.6 μg/mL) is superior to the commercial azoxystrobin (EC50 = 16.9 μg/mL) and close to fluopicolide (EC50 = 1.0 μg/mL). Initial structure–activity relationship (SAR) analysis showed that the heterocyclic piperidine group can influence the biological activities of the title compounds significantly. The fungicidal activity of compounds with piperidine is better than that of compounds without piperidine. The highly-active compound 3b, with its simple structure and easy synthetic route, is worthy to be further studied as a new lead fungicide. View Full-Text
Keywords: benzaldehyde; thiosemicarbazide; piperidine; synthesis; fungicidal activity benzaldehyde; thiosemicarbazide; piperidine; synthesis; fungicidal activity

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Zhang, X.; Lei, P.; Sun, T.; Jin, X.; Yang, X.; Ling, Y. Design, Synthesis, and Fungicidal Activity of Novel Thiosemicarbazide Derivatives Containing Piperidine Fragments. Molecules 2017, 22, 2085.

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