Novel Trifluoromethylpyrazole Acyl Thiourea Derivatives: Synthesis, Antifungal Activity and Docking Study

Author(s): Han Wang, Zhi-Wen Zhai, Yan-Xia Shi, Cheng-Xia Tan, Jian-Quan Weng, Liang Han, Bao-Ju Li, Xing-Hai Liu*.

Journal Name: Letters in Drug Design & Discovery

Volume 16 , Issue 7 , 2019

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Abstract:

Background: In recent years, pyrazole carboxamide derivatives possessed excellent fungicidal activity. In the process of designing new fungicides, the carboxamide group was modified in order to find novel structure pyrazole carboxamide derivatives.

Methods: Ten novel trifluoromethyl pyrazole acyl thiourea derivatives were designed and synthesized. In vivo fungicidal activities of these compounds were tested against Fusarium oxysporum, Corynespora mazei and Botrytis cinerea, respectively.

Results: Particularly compounds exhibited significant control effective at 100 mg/L. More importantly, some compounds showed the good control effective at 10 mg/L. Furthermore, docking was established to study the structure-activity relationship of the title compounds.

Conclusion: It is possible that trifluoromethylpyrazole acyl thiurea derivatives, which possess good control effective against Botrytis cinerea, may become novel lead compounds for the development of fungicides with further structure modification.

Keywords: Trifluoromethylpyrazole, thiourea, antifungal activity, docking, fusarium oxysporum, corynespora mazei, botrytis cinerea.

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Article Details

VOLUME: 16
ISSUE: 7
Year: 2019
Page: [785 - 791]
Pages: 7
DOI: 10.2174/1570180815666180704103047
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