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

徐志红; 董宏波; 韩金涛; 刘斌; 金淑惠; 王明安

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

doi: 10.3969/j.issn.1008-7303.2014.06.05

1.
中国农业大学应用化学系, 北京 100193
2.
长江大学农学院, 湖北荆州 434205

基金项目:

“十二五”国家科技支撑计划(2011BAE06B03).

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出版历程
- 收稿日期: 2014-09-01
- 修回日期: 2014-10-04
- 刊出日期: 2014-12-12

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

1.
Department of Applied Chemistry, China Agricultural University, Beijing 100193, China
2.
College of Agriculture, Yangtze University, Jingzhou 434205, Hubei Province, China

摘要

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%。
- 5-(4-氨基苯基/苄基)-2,4-咪唑啉二酮 /
- 芳基磺酰胺 /
- 合成 /
- 除草活性 /
- 杀菌活性
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.
- 5-(4-aminophenyl/benzyl)-hydantoin /
- arylsulfonamide /
- synthesis /
- herbicidal activity /
- fungicidal activity

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参考文献(22)

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