β-Lactamase inhibition profile of new amidine-substituted diazabicyclooctanes

The diazabicyclooctane (DBO) scaffold is the backbone of non-β-lactam-based second generation β-lactamase inhibitors. As part our efforts, we have synthesized a series DBO derivatives A1 – 23 containing amidine substituents at C2 position bicyclic ring. These compounds, alone and in combination with meropenem, were tested against ten bacterial strains for their antibacterial activity vitro. All compounds did not show when (MIC >64 mg/L), however, they exhibited moderate inhibition presence meropenem by lowering its MIC values. compound A12 proved most potent among other counterparts all species from <0.125 mg/L to 2 mg/L, comparable avibactam both E. coli value mg/L.