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.