Bicyclic Boronate ??Lactamase Inhibitors: The Present Hope against Deadly Bacterial Pathogens

The use of ?-lactamase inhibitors in combination with ?-lactam antibiotics is an emerging area drug discovery. This strategy allows the restoration therapeutic efficacy these clinical against multiresistant bacteria. These pathogens are resistant because they express enzymes, which prevent antibiotic action by catalyzing hydrolysis ring. enzymes quite diverse both their structural architecture and hydrolytic capability, as well mechanism action. ever-increasing emergence that capable coproducing different types ?-lactamases has triggered search for ultrabroad-spectrum deactivating serine- metallo-?-lactamases. A recent breakthrough this long-pursued unmet need discovery bicyclic boronate inhibitors, specifically taniborbactam, VNRX-7145, QPX7728, currently under development cefepime, ceftibuten, QPX2014, respectively. present article highlights potential spectrum compared those other ?-lactam/?-lactamase inhibitor combinations recently approved food administration. molecular basis activity boron-based also discussed, on available crystal structures results computational studies.