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

文献类型： 外文期刊

第一作者： Wang, Han

作者： Wang, Han;Zhai, Zhi-Wen;Tan, Cheng-Xia;Weng, Jian-Quan;Han, Liang;Liu, Xing-Hai;Liu, Xing-Hai;Shi, Yan-Xia;Li, Bao-Ju

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关键词： Trifluoromethylpyrazole; thiourea; antifungal activity; docking; fusarium oxysporum; corynespora mazei; botrytis cinerea

期刊名称：LETTERS IN DRUG DESIGN & DISCOVERY （ 影响因子：1.15； 五年影响因子：0.994 ）

ISSN： 1570-1808

年卷期： 2019 年 16 卷 7 期

页码：

收录情况： SCI

摘要： 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.

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