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Molecules 2014, 19(9), 14036-14051; doi:10.3390/molecules190914036

Design, Synthesis and Fungicidal Activities of Some Novel Pyrazole Derivatives

Research & Development Center of Biorational Pesticide, Key Laboratory of Plant Protection Resources and Pest Management of Ministry of Education, Northwest A&F University, Xinong Road 22, Yangling 712100, Shaanxi, China
These authors contributed equally to this work.
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Author to whom correspondence should be addressed.
Received: 7 August 2014 / Revised: 1 September 2014 / Accepted: 2 September 2014 / Published: 8 September 2014
(This article belongs to the Section Organic Synthesis)
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Abstract

In order to discover new compounds with good fungicidal activities, 32 pyrazole derivatives were designed and synthesized. The structures of the target compounds were confirmed by 1H-NMR, 13C-NMR, and high-resolution electrospray ionization mass spectrometry (HR-ESI-MS), and their fungicidal activities against Botrytis cinerea, Rhizoctonia solani Kuhn, Valsa mali Miyabe et Yamada, Thanatephorus cucumeris (Frank) Donk, Fusarium oxysporum (S-chl) f.sp. cucumerinum Owen, and Fusarium graminearum Schw were tested. The bioassay results indicated that most of the derivatives exhibited considerable antifungal activities, especially compound 26 containing a p-trifluoromethyl- phenyl moiety showed the highest activity, with EC50 values of 2.432, 2.182, 1.787, 1.638, 6.986, and 6.043 μg/mL against B. cinerea, R. solani, V. mali, T. cucumeris, F. oxysporum, and F. graminearum, respectively. Moreover, the activities of compounds such as compounds 2732 were enhanced by introducing isothiocyanate and carboxamide moieties to the 5-position of the pyrazole ring. View Full-Text
Keywords: pyrazole derivatives; chemical modification; antifungal activity; structure–activity relationships pyrazole derivatives; chemical modification; antifungal activity; structure–activity relationships
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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Liu, X.-R.; Wu, H.; He, Z.-Y.; Ma, Z.-Q.; Feng, J.-T.; Zhang, X. Design, Synthesis and Fungicidal Activities of Some Novel Pyrazole Derivatives. Molecules 2014, 19, 14036-14051.

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