Side chain SAR of bicyclic β-lactamase inhibitors (BLIs). 1. Discovery of a class C BLI for combination with imipinem

Bridged monobactam β-lactamase inhibitors were prepared and evaluated as potential partners for combination with imipenem to overcome class C β-lactamase mediated resistance. The (S)-azepine analog 2 was found to be effective in both in vitro and in vivo assays and was selected for preclinical development.

Bridged monobactam β-lactamase inhibitors were prepared and evaluated as potential partners for combination with imipenem to overcome class C β-lactamase mediated resistance. The (S)-azepine analog 2 was found to be effective in both in vitro and in vivo assays and was selected for preclinical development.Figure optionsDownload as PowerPoint slide