徐志红, 董宏波, 韩金涛, 刘斌, 金淑惠, 王明安. 5-(4-氨基苯基/苄基)-2,4-咪唑啉二酮芳基磺酰胺的合成及其生物活性[J]. 农药学学报, 2014, 16(6): 659-666. DOI: 10.3969/j.issn.1008-7303.2014.06.05
    引用本文: 徐志红, 董宏波, 韩金涛, 刘斌, 金淑惠, 王明安. 5-(4-氨基苯基/苄基)-2,4-咪唑啉二酮芳基磺酰胺的合成及其生物活性[J]. 农药学学报, 2014, 16(6): 659-666. DOI: 10.3969/j.issn.1008-7303.2014.06.05
    XU Zhihong, DONG Hongbo, HAN Jintao, LIU Bin, JIN Shuhui, WANG Ming'an. Synthesis and biological activity of 5-(4-aminophenyl/benzyl)-hydantoin arylsulfonamide[J]. Chinese Journal of Pesticide Science, 2014, 16(6): 659-666. DOI: 10.3969/j.issn.1008-7303.2014.06.05
    Citation: XU Zhihong, DONG Hongbo, HAN Jintao, LIU Bin, JIN Shuhui, WANG Ming'an. Synthesis and biological activity of 5-(4-aminophenyl/benzyl)-hydantoin arylsulfonamide[J]. Chinese Journal of Pesticide Science, 2014, 16(6): 659-666. DOI: 10.3969/j.issn.1008-7303.2014.06.05

    5-(4-氨基苯基/苄基)-2,4-咪唑啉二酮芳基磺酰胺的合成及其生物活性

    Synthesis and biological activity of 5-(4-aminophenyl/benzyl)-hydantoin arylsulfonamide

    • 摘要: 以5-(4-氨基苯基/苄基)-2,4-咪唑啉二酮为原料,在三乙胺或吡啶作傅酸剂的条件下与取代磺酰氯反应,得到44个新的5-(4-氨基苯基/苄基)-2,4-咪唑啉二酮芳基磺酰胺类化合物,其结构均经1H NMR、HR-MS和元素分析确证。初步生物活性测试结果表明,部分化合物对供试植物病原菌和稗草Echinochloa crusgalli显现出一定的抑制活性,其中化合物 4p 和 4u 在50 μg/mL下对油菜菌核病菌Sclerotinia scleotiorum的抑制率分别为76.0%和75.2%,化合物 3j 在100 μg/mL下对稗草生长的抑制率为50%。

       

      Abstract: Forty-four novel 5-(4-aminophenyl/benzyl)-hydantoinarylsulfonamides were prepared using 5-(4-aminophenyl/benzyl)-hydantoins and substituted phenylsulfonyl chlorides as raw materials. Their structures were confirmed by 1H NMR, HR-MS, and elementary analysis. Preliminary bioassay results showed that some products possessed certain fungicidal and herbicidal activities. At the concentration of 50 μg/mL, inhibition rate of compound 4p and 4u against Sclerotinia scleotiorum was 76.0% and 75.2% respectively. Compound 3j exhibited an inhibition rate of 50% against Echinochloa crusgalli at the concentration of 100 μg/mL.

       

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