高等学校化学学报Issue(4)：672-681,10.DOI:10.7503/cjcu20140955
新型含苯基取代嘧啶基磺酰脲衍生物的设计、合成及生物活性
Design, Synthesis and Biological Activity of Novel Sulfonylurea Derivatives Containing Phenyl-substituted Pyrimidine Moiety
摘要
Abstract
Acetolactate synthase( ALS) has been regarded as an attractive target for fungicide and herbicide discovery. Furthermore, sulfonylurea( SU) as one of the most active ALS inhibitors were used as herbicides in crops protect. In order to discuss the multi-biological activity of SU, two series of novel SU derivatives contai-ning phenyl-substituted pyrimidine moiety were designed, synthesized and their antifungal activity and herbi-cidal activity were evaluated. The bioassay results indicated that some title compounds showed excellent anti-fungal activity against Physalospora piricola and Rhizoctonia cerealis in vitro at the dosage of 50 mg/L. Particu-larly, compound 9f exhibited more than 65% inhibitory activity against five phytopathogens. On the basis of advanced screening test, the EC50 value of compound 8f against P. piricola was 8. 63 mg/L, which was a little higher than Chlorothalonil(EC50=7. 33 mg/L), the EC50 value of compounds 8k(5. 48 mg/L) and 9k(6. 09 mg/L) against R. cerealis were similar to Chlorothalonil( EC50=4. 26 mg/L) . In addtion, the title compounds showed favorable pre-emergence treatment herbicidal activity against Brassica napus and Amaranthus retroflexus at the dosage of 75 g/ha. For example, compounds 8d and 9d showed 86% and 73% inhibition activity respectively against Brassica napus; compound 9 h exhibited 100% herbicidal activity against Amaranthus retroflexus, which was better than that of Chlorsulfuron ( 96%) . The results provided useful information for designing new SU with highly fungicidal activity and herbicidal activity.关键词
磺酰脲/乙酰乳酸合成酶/苯基取代嘧啶/抑菌活性/除草活性Key words
Sulfonylurea/Acetolactate synthase/Phenyl-subsituted pyrimidine/Antifungal activity/Herbicidal activity分类
化学化工引用本文复制引用
陈伟,魏巍,周莎,李永红,张晓,童军,李玉新,李正名..新型含苯基取代嘧啶基磺酰脲衍生物的设计、合成及生物活性[J].高等学校化学学报,2015,(4):672-681,10.基金项目
国家自然科学基金(批准号:21272129)和“十二五”国家科技支撑计划项目(批准号:2011BAE06B05)资助.覮 Supported by the National Natural Scinece Foundation of China(No.21272129) and the National Key Technologies Research and Develop-ment Program of China(No.2011BAE06B05) （批准号:21272129）
