VNRX-6315

VNRX-6315 is an early lead, non-β-lactam, cyclic benzo-oxaborinine penicillin-binding protein inhibitor (PBPi) discovered by Venatorx Pharmaceuticals as part of its boronate-based antibacterial program targeting multidrug-resistant Neisseria gonorrhoeae. It was designed as a hybrid molecule incorporating the side chain of cefoperazone, a potent inhibitor of N. gonorrhoeae penicillin-binding protein 2 (PBP2), appended to a benzo-oxaborinine core originally developed for β-lactamase inhibitors, yielding promising minimum inhibitory concentrations against wild-type N. gonorrhoeae and providing a starting point for subsequent structure–activity relationship optimization toward more potent analogs such as VNRX-6752, VNRX-6884, and VNRX-6958.[1]