Beta-lactamase

PhoPS is a photoactivatable β-lactamase inhibitor. Upon exposure to light, PhoPS releases the active β-lactamase inhibitor Sulbactam. This compound is capable of inhibiting the synthesis of bacterial cell walls and the formation of biofilms in Escherichia coli, thereby exhibiting antibacterial activity.

Piperacillin hydrate is a semisynthetic broad-spectrum β-lactam antibiotic. It exhibits potent bactericidal activity against Gram-negative bacteria and some Gram-positive bacteria by targeting penicillin-binding proteins. Piperacillin hydrate is frequently combined with the β-lactamase inhibitor Tazobactam for enhanced efficacy.

Metallo-β-lactamase-IN-16 (compound 18), a sulfone-containing metallo-β-lactamase inhibitor, exhibits antimicrobial activity. It effectively inhibits various metallo-β-lactamases, including NDM-1 (New Delhi metallo-β-lactamase-1), IMP-1 (imipenemase-1), VIM-1 (Verona Integron-encoded Metallo-β-lactamase), and VIM-2. The IC50 values for these enzymes are 0.16 nM, 0.23 nM, 0.31 nM, and 1.0 nM respectively.

epi-D-Captopril (epi-D-SQ 14225) is a stereoisomer of Captopril and functions as an inhibitor of metallo-beta-lactamases (MBLs). The IC50 values of epi-D-Captopril for NDM-1, IMP-1, and VIM-2 are 64 μM, 173 μM, and 5.5 μM, respectively. This compound holds potential for research in MBLs-related antibiotic-resistant infections.

Carpetimycin D exhibits potent activity against both Gram-positive and Gram-negative bacteria, including those that produce β-lactamase. Additionally, Carpetimycin D strongly inhibits β-lactamase.

NDM-1 inhibitor-8 (Compound 18b) is a covalent inhibitor of New Delhi metallo-β-lactamase-1 (NDM-1), with an IC50 of 7.03 μM. It effectively inhibits resistant bacterial strains and demonstrates synergistic antibacterial effects when used in combination with Meropenem. In mouse models, NDM-1 inhibitor-8 exhibits anti-infective activity.

Carpetimycin A exhibits potent activity against both Gram-positive and Gram-negative bacteria, including those that produce β-lactamase. It also acts as a strong inhibitor of β-lactamase.

Carpetimycin C exhibits strong activity against both Gram-positive and Gram-negative bacteria, including those that produce β-lactamase. It also has a powerful inhibitory effect on β-lactamase .

Carpetimycin B exhibits potent activity against both Gram-positive and Gram-negative bacteria, including those that produce β-lactamase. Carpetimycin B is also a strong inhibitor of β-lactamase (β-lactamase).

Doxazosin impurity 12 acts as an inhibitor of CTX-M β-lactamase (Beta-lactamase) with a Ki value of 0.7 mM against CTX-M.

Dotriacolide is a β-lactamase inhibitor with notable inhibitory activity against penicillinase and cephalosporinase, displaying ID50 values of 0.61 μg/mL and 0.15 μg/mL respectively. It holds potential for research in infectious diseases.

Izumenolide exhibits inhibitory effects on certain β-lactamases, with an IC50 concentration of 0.01 μg/mL specifically for TEM-2 β-lactamase.

Xeruborbactam isoboxil is a β-lactamase (beta-lactamase) inhibitor.

NDM-1 inhibitor-7 (Compound A8) is an NDM-1 inhibitor with an IC50 of 10.284 μM. It restores the ability of meropenem (MEM) to penetrate the cell wall of Gram-negative bacteria and effectively reinstates MEM's antibacterial activity against NDM-1 positive Escherichia coli. Moreover, NDM-1 inhibitor-7 demonstrates significant efficacy in both Galleria mellonella and murine peritonitis infection models.

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.