期刊论文

中文

农药学学报

1008-7303

2017

19

4

418-427

10.16801/j.issn.1008-7303.2017.0055

21372093,201203022:公益性行业(农业)科研专项 21372093:国家自然科学基金 21672079:国家自然科学基金

本校为其他机构

对羟基苯基丙酮酸双加氧酶(HPPD)是一种重要的除草剂作用靶标。为了发现具有高活性和高选择性的新型HPPD抑制型除草剂,对前期合成的23个含咪唑啉酮结构单元的吡唑类衍生物(2A~2W)进行了深入的生物活性评价和构效关系研究,比较了它们对拟南芥HPPD(AtHPPD)和人源HPPD(hHPPD)抑制活性的差异,从酶水平上总结了该类化合物的结构-活性关系和种属选择性规律,从活体植株水平研究了它们的除草活性。结果表明:部分化合物表现出良好的除草活性和作物安全性,其中化合物2E和2G在150 g/hm~2剂量下对荠菜、繁缕、小藜和棒头草抑制活性达到80%以上,且其对作物的安全性也明显优于商品化除草剂硝磺草酮。此外,化合...

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 comp...