Design, Synthesis, and Herbicidal Activity Evaluation of Novel Aryl-Naphthyl Methanone Derivatives

2019 
4-Hydroxyphenylpyruvate dioxygenase is one of the most vital targets for herbicides discovery. In search for HPPD inhibitors with novel scaffolds, a series of aryl-naphthyl methanone derivatives have been designed and synthesized through alkylation and Friedel-Crafts acylation reactions. The bioassay indicated some of these compounds displayed preferable herbicidal activity at the rate of 0.75 mmol/m2 by post-emergence application, in which compound 3h displayed the best herbicidal activity. The molecular docking showed that the binding pattern of compound 3h with HPPD. This study showed that aryl-naphthyl methanone derivatives could be a potential lead structure for further development of novel herbicides.
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