Novel HPPD inhibitors: triketone 2H‐benzo[b][1,4]oxazin‐3(4H)‐one analogs
2018
Li, Hua‐Bin | Li, Lei | Li, Jun‐Xian | Han, Ting‐Feng | He, Jing‐Li | Zhu, You‐Quan
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. © 2017 Society of Chemical Industry
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