Shielding Metabolic Hotspots in the Triketone-Quinoline Scaffold Yields Potent 4-Hydroxyphenylpyruvate Dioxygenase Inhibitors.
4-Hydroxyphenylpyruvate dioxygenase (HPPD; EC 1.13.11.27) is an important target for modern herbicide discovery. To translate HPPD inhibitors into effective herbicide candidates, we developed a metabolism-oriented design strategy to improve the in vivo efficacy of triketone-quinoline HPPD inhibitors. By shielding the m...