Structure-Guided Discovery of Benzothiazinone-Triketone Hybrids as Novel Subnanomolar 4-Hydroxyphenylpyruvate Dioxygenase Inhibitors | Synapse
June 4, 2026
Structure-Guided Discovery of Benzothiazinone-Triketone Hybrids as Novel Subnanomolar 4-Hydroxyphenylpyruvate Dioxygenase Inhibitors
Key Points
The aim is to identify new 4-hydroxyphenylpyruvate dioxygenase inhibitors using structure-guided discovery techniques.
Structure-guided design of benzothiazinone-triketone hybrids.
Evaluation of inhibitory potency against 4-hydroxyphenylpyruvate dioxygenase.
Identified a hybrid compound with an IC50 of 4.56 nM, the most potent HPPD inhibitor reported to date.
Abstract
= 4.56 nM) and was regarded as the most potent HPPD inhibitor to date. These results demonstrate that the triketone-benzothiazinone hybrid is a potential scaffold for discovering new HPPD inhibitors.