5 years ago

Novel HPPD inhibitors: Triketone 2H-benzo[b][1,4]oxazin-3(4H)-one analogs

Jing-Li He, Hua-Bin Li, Ting-Feng Han, Jun-Xian Li, You-Quan Zhu, Lei Li
BACKGROUND Herbicides that inhibit 4-hydroxyphenylpyruvate dioxygenase (HPPD, EC are very important for grass weed control. In order to discover novel HPPD herbicides with herbicidal activity, a series of triketone 2H-benzo[b][1,4]oxazin-3(4H)-one analogs were 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, such as B39 (IC50 = 0.172 μM) and B41 (IC50 = 0.156 μM). In addition, some of these compounds exhibited pre-emergence 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 further development of novel HPPD herbicides.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1002/ps.4739

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