Metallo-β-lactamase-IN-5 (compound 5c) is a potent metallo-β-lactamases (MBL) inhibitor. Metallo-β-lactamase-IN-5 shows inhibitory activity against MBLs NDM-1 and VIM-1. Metallo-β-lactamase-IN-5 inhibits HUVECs with an IC 50 of 45 μg/mL. Metallo-β-lactamase-IN-5 plus Imipenem exhibits synergistic antimicrobial activity.