新型含二甲氧基甲基嘧啶基磺酰脲衍生物的合成及生物活性  

Design,Synthesis and Biological Activity of Novel Sulfonylurea Derivatives Containing Dimethoxymethyl-substituted Pyrimidine Moiety

作　　者：陈伟[1] 魏巍[1] 刘明[1] 华学文[1] 李玉新[1] 李永红[1] 张晓[1] 李正名[1] 

机构地区：[1]南开大学元素有机化学国家重点实验室化学化工协同创新中心(天津),天津300071

出　　处：《高等学校化学学报》2015年第7期1291-1297,共7页Chemical Journal of Chinese Universities

基　　金：国家自然科学基金(批准号:21272129);'十二五'国家科技支撑计划项目(批准号:2011BAE06B05);高等学校学科创新引智计划(批准号:B06005)资助~~

摘　　要：将二甲氧基甲基引入到嘧啶环的4位,设计并合成了15个结构新颖的磺酰脲类衍生物.初步生物活性测试结果表明,目标化合物具有较好的除草活性.在75 g/ha的剂量下,化合物6a和6g对油菜的芽前除草活性为100%,与对照药单嘧磺隆和氯磺隆相当;在50 mg/L的浓度下,化合物6i和6o对3种病菌的离体抑制率都超过80%,与对照药百菌清和多菌灵接近.Sulfonylureas（SUs） as one of the most active herbicides targeted on acetolactate synthase（ALS）. ALS was found not only in plants, but also in fungi and bacteria. In order to study the multi-biological activity of sulfonylurea（ SU）, a series of novel SU derivatives containing dimethoxymethyl pyrimidine moiety was de- signed, synthesized according to bioisosteric principles. The bioassay results indicated that the title compounds exhibited favorable herbicidal activity. Compounds 6a and 6g showed 100% pre-emergence inhibition activity against Brassica napus at the dosage of 75 g/ha, which were near to that of Monosulfuron and Chlorsulfuron （ 100% ）. In addtion, some and 60 showed over 80% an of the title compounds also exhibited moderate antifungal activity. Compounds 6i tifungal activity against three fungi in vitro at the concentration of 50 mg/L, and closed to that of Chlorothalonil and Carbendazim. It provided useful information for designing new SU with highly herbicidal activity and fungicidal activity.

关 键 词：磺酰脲 二甲氧基甲基 乙酰乳酸合成酶 除草活性 抑菌活性 

分 类 号：O625.7[理学—有机化学]