molecules of the month

ETX0282 is an oral prodrug of a class A, C, and D serine β-lactamase inhibitor in clinical development for drug-resistant enterobacterial infections in combination with the beta-lactam drug cefpodoxime proxetil. Impressively ETX0282 had no observed adverse effect levels (NOAELs) of 500 mg/kg/day and 400 mg/kg/day in rat and dog, respectively, despite the reactive-looking nature of the strained bridged carbamate core and the monofluoroether. I was surprised by the chemical stability of the fluoroether moiety, which can be seen in the co-crystal structure.