农药学学报2017，Vol.19Issue(4)：418-427,10.DOI:10.16801/j.issn.1008-7303.2017.0055
含咪唑啉酮结构的吡唑类对羟基苯基丙酮酸双加氧酶抑制剂的除草活性及选择性研究
Herbicidal activity and selectivity profiles of imidazole ketone-containing p-hydroxyphenylpyruvate dehydrogenase inhibitors
摘要
Abstract
p-Hydroxyphenylpyruvate dehydrogenase (HPPD) is an important target in herbicide discovery. In order to discover new HPPD inhibitor-based herbicide with high activity and selectivity, the comprehensive bioevaluation of our previously synthesized imidazole ktone-containing HPPD inhibitors was conducted and the structure-activity relationship was studied. More specifically, the in vitro inhibitory activities against Arabidopsis thaliana HPPD (AtHPPD) and human HPPD (hHPPD) were studied and the selectivity profile was evaluated. Their herbicidal activities in plants were then evaluated. Some compounds showed high HPPD enzyme inhibition activities and herbicidal activities. Especially, the compounds 2E and 2G exhibited good control effect toward broadleaf weeds in winter field at the dose of 150 g/hm2. More importantly, their crop safety profiles is superior to the commercial herbicide mesotrione. In addition, compound 2P exhibited excellent selectivity (about 93 times) that is about 23-fold higher than that of mesotrione, which showing a good application potential.关键词
咪唑啉酮/对羟基苯基丙酮酸双加氧酶/除草剂/除草活性/作物安全性Key words
imidazole ketone/p-hydroxyphenylpyruvate dehydrogenase/herbicide/herbicidal activity/crop safety分类
农业科技引用本文复制引用
徐玉玲,林红艳,吴丰旭,康德来,杨文超,杨光富..含咪唑啉酮结构的吡唑类对羟基苯基丙酮酸双加氧酶抑制剂的除草活性及选择性研究[J].农药学学报,2017,19(4):418-427,10.基金项目
国家公益性行业 (农业) 科研专项 (21372093, 201203022) （农业）
国家自然科学基金 (21372093, 21672079). （21372093, 21672079）
