GyrB-ParE Dual Target

Previous studies have demonstrated that potent antibacterial agents can be generated using SBDD techniques by targeting both GyrB and ParE. While these efforts were successful in generating compounds of high antibacterial potency, the initial leads suffered from poor solubility and high serum binding. At Trius, we have applied our fragment-based lead generation approach to identify more soluble drug-like leads. We are currently optimizing these leads to generate compounds with improved solubility, less serum binding and improved spectrum.