β lactamase in 5

β-Lactamase-IN-5, a β-lactamase inhibitor isolated from compound 720, holds significant potential for studying bacterial infections.

Metallo-β-lactamase-IN-5 (compound 5c) is a potent inhibitor of metallo-β-lactamases (MBLs), demonstrating inhibitory activity against MBLs NDM-1 and VIM-1. It effectively inhibits HUVECs with an IC50 value of 45 μg mL. Additionally, when combined with Imipenem, Metallo-β-lactamase-IN-5 exhibits synergistic antimicrobial activity [1].

MBL-IN-5 is an inhibitor of metallo-β-lactamase (MBL). It effectively suppresses three clinically significant B1 subfamily MBLs: NDM-1, VIM-1, and IMP-1 with IC50 values of 0.05 nM, 14 nM, and 21 nM respectively. MBL-IN-5 notably enhances the efficacy of carbapenem antibiotics against MBL-producing clinical strains and, when combined with IPM antibiotics, significantly reduces bacterial load in a thigh infection model.

Metallo-β-lactamase-IN-6 is a highly effective inhibitor of VIM-Type metallo-β-lactamase, demonstrating IC50 values of 0.56 μM, 29.50 μM, and 5.78 μM for VIM-2, VIM-1, and VIM-5, respectively. Additionally, Metallo-β-lactamase-IN-6 exhibits potent synergistic antibacterial properties when combined with Meropenem, particularly against engineered Escherichia coli strains and clinically isolated Pseudomonas aeruginosa carrying the VIM-2 MBL gene [1].

Metallo-β-lactamase-IN-7 is a potent inhibitor of VIM-type metallo-β-lactamase with IC50 values of 0.019 μM, 13.64 μM, and 0.38 μM for VIM-2, VIM-1, and VIM-5, respectively. Metallo-β-lactamase-IN-7 also enhances the antibacterial activity of Meropenem against Gram-negative bacterial strains [1].