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Amino acid-oriented poly-substituted heterocyclic tetramic acid derivatives as potential antifungal agents

文献类型： 外文期刊

作者： Wang, Shuangshuang 1 ; Bao, Longzhu 1 ; Song, Di 1 ; Wang, Jingjing 1 ; Cao, Xiufang 1 ; Ke, Shaoyong 2 ;

作者机构： 1.Huazhong Agr Univ, Coll Sci, Wuhan 430070, Hubei, Peoples R China

2.Hubei Acad Agr Sci, Natl Biopesticide Engn Res Ctr, Hubei Biopesticide Engn Res Ctr, Wuhan 430064, Hubei, Peoples R China

关键词： Tetramic acid; Synthesis; Antifungal activities; Plant pathogenic fungus; Fungicides

期刊名称：EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY （ 影响因子：6.514； 五年影响因子：6.099 ）

ISSN： 0223-5234

年卷期： 2019 年 179 卷

页码：

收录情况： SCI

摘要： In order to find new potential pesticide molecules with antifungal activities, we have designed and synthesized a series of amino acid-oriented poly-substituted tetramic acid derivatives, and evaluated their potential antifungal activities against six kinds of plant pathogenic fungus commonly found in agriculture systematically, including Phomopsis adianticola, Fusarium graminearum, Alternaria tennis Nees, Magnaporthe oryzae, Gloeosporium theae-sinensis, Sclerotinia sclerotiorum. According to the preliminary bioassay studies, all tested molecules, especially compounds I-2, I-5, I-12, I-15, exhibited significant and broad-spectrum anti-fungal effect in vitro compared to the intermediates M-1, M-2, M-3 and hymexazol. What's more, the inhibition rate of compounds I-5, I-6, I-15 against Phomopsis adianticola reached 74.42%, 60.33%, 65.21%, as well as compounds I-3, I-5, I-15 against Sclerotinia sclerotiorum were 65.65%, 74.92%, 61.36%. Further investigation results indicated that compounds I-2, I-5, I-15 presented obviously inhibitory activities against Phomopsis adianticola compared with hymexazol, which might be considered as the basic active framework for further potential fungicides discovery. (C) 2019 Elsevier Masson SAS. All rights reserved.

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