Development of Protoporphyrinogen IX Oxidase Inhibitors for Sustainable Agriculture

Agrochemicals are essential to sustainable agricultural development. Protoporphyrinogen oxidase (PPO, EC 1.3.3.4) is an important target for agrochemical research. Currently, more than 31 PPO inhibitors have been launched into the market as crop protection products. These compounds have many advantages, such as low toxicity, low application-rate, broad-spectrum of weeds control, and environmentally benign characteristics. The past six decades have witnessed remarkable achievements in the development of PPO inhibitors. Many compounds with diverse structures were designed and synthesized. Based on increasing knowledge of the biochemistry of PPO and computer-aided modeling and design (CAMD), we continue to uncover exciting prospects for novel molecules targeting PPO. In this chapter, we summarize the current knowledge on the molecular mechanism of PPO, the molecular interactions between inhibitors and PPOs, structure-activity relationships (SAR) of PPO inhibitors, and recent efforts on the discovery of PPO inhibitors for crop protection.