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

作　　者：徐志红[1,2] 董宏波[1] 韩金涛[1] 刘斌[1] 金淑惠[1] 王明安[1] 

机构地区：[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

出　　处：《农药学学报》2014年第6期659-666,共8页Chinese Journal of Pesticide Science

基　　金："十二五"国家科技支撑计划(2011BAE06B03)

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 NM R、HR-M S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50μg/m L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100μg/m L下对稗草生长的抑制率为50%。Forty-four novel 5-（ 4-aminophenyl / benzyl）-hydantoinarylsulfonamides w ere prepared using5-（ 4-aminophenyl / benzyl）-hydantoins and substituted phenylsulfonyl chlorides as raw materials. Their structures w ere confirmed by1 H NM R,HR-M S,and elementary analysis. Preliminary bioassay results show ed that some products possessed certain fungicidal and herbicidal activities. At the concentration of50 μg / m L,inhibition rate of compound 4p and 4u against Sclerotinia scleotiorum w as 76. 0% and75. 2% respectively. Compound 3j exhibited an inhibition rate of 50% against Echinochloa crusgalli at the concentration of 100 μg / m L.

关 键 词：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 

分 类 号：S482.26[农业科学—农药学] S482.46[农业科学—植物保护]