丁成荣, 殷许, 潘亚运, 张国富, 魏军, 谭成侠. 含哌啶噻唑结构的乙酰氨基衍生物的合成及杀菌活性[J]. 农药学学报, 2019, 21(3): 372-377. DOI: 10.16801/j.issn.1008-7303.2019.0045
    引用本文: 丁成荣, 殷许, 潘亚运, 张国富, 魏军, 谭成侠. 含哌啶噻唑结构的乙酰氨基衍生物的合成及杀菌活性[J]. 农药学学报, 2019, 21(3): 372-377. DOI: 10.16801/j.issn.1008-7303.2019.0045
    DING Chengrong, YIN Xu, PAN Yayun, ZHANG Guofu, WEI Jun, TAN Chengxia. Synthesis and fungicidal activity of acetamido derivatives containing piperidine thiazole moiety[J]. Chinese Journal of Pesticide Science, 2019, 21(3): 372-377. DOI: 10.16801/j.issn.1008-7303.2019.0045
    Citation: DING Chengrong, YIN Xu, PAN Yayun, ZHANG Guofu, WEI Jun, TAN Chengxia. Synthesis and fungicidal activity of acetamido derivatives containing piperidine thiazole moiety[J]. Chinese Journal of Pesticide Science, 2019, 21(3): 372-377. DOI: 10.16801/j.issn.1008-7303.2019.0045

    含哌啶噻唑结构的乙酰氨基衍生物的合成及杀菌活性

    Synthesis and fungicidal activity of acetamido derivatives containing piperidine thiazole moiety

    • 摘要: 为了寻找高效的杀菌活性物质,以哌啶噻唑结构为母体,甘氨酸为连接基团,通过重氮化、氯化、成环和缩合等步骤合成了14个含哌啶噻唑结构的乙酰氨基衍生物,通过核磁共振氢谱 (1H NMR)、碳谱(13C NMR)及高分辨质谱 (HRMS)对化合物的结构进行确证。初步杀菌活性测定结果表明:甘氨酸作为连接基团对化合物杀菌活性的提高具有积极影响,其中,化合物 7a7c7g 在25 mg/L剂量下对黄瓜灰霉病菌的抑制率为68.7%、71.6%和67.2%,化合物 7a7g7i 对马铃薯晚疫病菌的抑制率分别为50.8%、61.9% 和55.8%。

       

      Abstract: In order to find novel compounds with high fungicidal activities, a series of acetamido derivatives containing piperidine thiazole moiety were designed and synthesized by the procedure of diazotization, chlorination, cyclization and condensation. Their structures were characterized by 1H NMR, 13C NMR and HRMS. Preliminary bioassay indicated that some title compounds showed good fungicidal activities and the introduction of acetamido group had positive effect on the fungicidal activity. At the concentration of 25 mg/L, compounds 7a , 7c and 7g possessed fungicidal activities against Botrytis cinereal with the inhibition rates of 68.7%, 71.6% and 67.2%, respectively. In addition, compounds 7a , 7g and 7i showed good fungicidal activities against Phytophthora infestans (Mont.) de Bary with the inhibition rate of 50.8%, 61.9% and 55.8%, respectively.

       

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