Synthesis and herbicidal activities of aryloxyacetic acid derivatives as HPPD inhibitors.

A series of aryloxyacetic acid derivatives were designed and synthesized as 4-hydoxyphenylpyruvate dioxygenase (HPPD) inhibitors. Preliminary bioassay results reveal that these derivatives are promising HPPD (HPPD) inhibitors, in particular compounds ( = 0.011 µM) and ( = 0.012 µM), which exhibit similar activities to that of mesotrione, a commercial HPPD herbicide ( = 0.013 µM). Furthermore, the newly synthesized compounds show significant greenhouse herbicidal activities against tested weeds at dosages of 150 g ai/ha. In particular, exhibited high herbicidal activity for pre-emergence treatment that was slightly better than that of mesotrione. In addition, compound was safe for weed control in maize fields at a rate of 150 g ai/ha, and was identified as the most potent candidate for a novel HPPD inhibitor herbicide. The compounds described herein may provide useful guidance for the design of new HPPD inhibiting herbicides and their modification.