Syntheses, biological activities and SAR studies of novel carboxamide compounds containing piperazine and arylsulfonyl moieties

文献类型： 外文期刊

第一作者： Wang, Bao-Lei

作者： Wang, Bao-Lei;Zhang, Shu-Jun;Ma, Yi;Wang, Hong-Xue;Zhang, Li-Yuan;Wei, Wei;Liu, Xing-Hai;Li, Yong-Hong;Li, Zheng-Ming;Shi, Yan-Xia;Li, Bao-Ju

作者机构：

关键词： Piperazine derivatives;Arylsulfonyl group;Biological activities;3D-QSAR;Theoretical calculation

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

ISSN：

年卷期：

页码：

收录情况： SCI

摘要： A series of novel carboxamide compounds 19a-19j, 20a-20j and 22a-22d containing piperazine and arylsulfonyl moieties have been synthesized. The bioassay results showed that some compounds exhibited favorable herbicidal activities against dicotyledonous plants and many of them possessed excellent antifungal activities. Among 24 novel compounds, some showed superiority over the commercial fungicides Chlorothalonil, Dimethomorph, Thiophanate-methyl, Iprodione, and Zhongshengmycin at 500 mg/L concentration. Some compounds also exhibited high KARI inhibitory activity at 100 mu g/mL concentration and could be used as new KARI lead inhibitors for further studies. Moreover, SAR of these new compounds were comprehensively investigated using different computational methods in which 3D-QSAR model obtained provided useful information for further structural optimization for the discovery of new fungicides. The results of this research will contribute to explore comprehensive biological activities of piperazine-containing compounds in different areas of chemistry. (C) 2016 Elsevier Masson SAS. All rights reserved.

分类号： R9

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