Hua-Bin Li1,2, Lei Li1, Jun-Xian Li1, Ting-Feng Han1, Jing-Li He1, You-Quan Zhu1. 1. State Key Laboratory of Elemento-organic Chemistry, College of Chemistry, Nankai University, Tianjin, China. 2. National Pesticide Engineering Research Center (Tianjin), College of Chemistry, Nankai University, Tianjin, China.
Abstract
BACKGROUND: Herbicides that inhibit 4-hydroxyphenylpyruvate dioxygenase (HPPD, EC 1.13.11.27) are very important for grass weed control. In order to discover novel HPPD herbicides, a series of triketone 2H-benzo[b] oxazin-3(4H)-one analogs was designed and synthesized. RESULTS: In comparison with the commercial triketone HPPD herbicide mesotrione (IC50 = 0.252 μM), some of these new triketone analogs displayed excellent HPPD inhibitory potency in vitro, for example B39 (IC50 = 0.172 μM) and B41 (IC50 = 0.156 μM). In addition, some of these compounds exhibited pre- and post-emergence herbicidal activity similar to mesotrione when applied at 375 g/ha. CONCLUSION: Many of the title compounds described in this paper could be important lead structures for the further development of novel HPPD herbicides.
BACKGROUND: Herbicides that inhibit 4-hydroxyphenylpyruvate dioxygenase (HPPD, EC 1.13.11.27) are very important for grass weed control. In order to discover novel HPPD herbicides, a series of triketone 2H-benzo[b] oxazin-3(4H)-one analogs was designed and synthesized. RESULTS: In comparison with the commercial triketoneHPPD herbicide mesotrione (IC50 = 0.252 μM), some of these new triketone analogs displayed excellent HPPD inhibitory potency in vitro, for example B39 (IC50 = 0.172 μM) and B41 (IC50 = 0.156 μM). In addition, some of these compounds exhibited pre- and post-emergence herbicidal activity similar to mesotrione when applied at 375 g/ha. CONCLUSION: Many of the title compounds described in this paper could be important lead structures for the further development of novel HPPD herbicides.
Authors: Anatoli V Lygin; Shiv S Kaundun; James A Morris; Eddie Mcindoe; Andrea R Hamilton; Dean E Riechers Journal: Front Plant Sci Date: 2018-11-21 Impact factor: 5.753