beta-lactam

Clavulanate lithium (Clavulanic acid lithium) is an inhibitor of β-lactamase.

Metallo β-lactamase ligand 1 is an inhibitor of class B β-lactamase exhibiting antibacterial activities.

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

BRL-42715 is an effective inhibitor of bacterial beta-lactamases.

β-Lactamase-IN-1 (4-(1,3-dihydroxypropan-2-yl)-6-methoxypyrido[2,3-b]pyrazin-3-one) is a β-Lactamase inhibitor and targets the infection of Neisseria gonorrhoeae.

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.

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.

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.

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.

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.

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.

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.

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.

MBL-IN-6 (Compound 6d) is a metal-β-lactamase (MBL) inhibitor with Ki values of 2.6 μM for NDM-1 and 0.08 μM for VIM-2. It acts synergistically with Imipenem against clinical isolates producing MBL, such as E. coli SI-M001, K. pneumoniae T2301, and S. marcescens SI-1591, with a MIC ranging from 2-64 μg/mL. MBL-IN-6 does not induce off-target effects and exhibits no inhibitory activity against ACE-1. This compound is useful for research on antibiotic resistance.

NDM-1-IN-10 (Compound CS-23) is an irreversible covalent inhibitor of New Delhi metallo-β-lactamase-1 (NDM-1) with an IC50 of 36 nM. It displays synergistic effects with Meropenem against E. coli expressing NDM-1, with a minimum inhibitory concentration (MIC) of 0.25 μg/mL for E. coli BL21/pET15b-blaNDM-1. NDM-1-IN-10 is applicable in bacterial infection research.

β-Lactamase-IN-11 is a β-lactamase (β-Lactamase) inhibitor with an IC50 of 30.37 μM. It exhibits significant antibacterial activity against Staphylococcus aureus and Pseudomonas aeruginosa, indicating its potential for addressing various resistant bacterial strains. β-Lactamase-IN-11 can be employed in research on infections caused by enzyme-producing resistant bacteria.

NDM-1-IN-11 is a potent covalent inhibitor of NDM-1 with an IC50 of 1.12 μM, acting by forming a Se-S bond with the enzyme. In both in vivo and in vitro models, NDM-1-IN-11, when combined with Meropenem, effectively inhibits the growth of NDM-1-producing E. coli. This compound is suitable for research addressing bacterial resistance caused by NDM-1.

NDM-1-IN-12 (Compound 10c) is an inhibitor of NDM-1 metallo-β-lactamase, exhibiting an IC50 value of 9 nM. It effectively reverses bacterial resistance to β-lactam antibiotics and shows a synergistic effect when used in combination with antibiotics and SBL inhibitors. NDM-1-IN-12 is utilized in research on combating multidrug-resistant bacteria.

rel-Avibactam (NXL-104) sodium is a β-lactamase inhibitor with broad-spectrum antibacterial activity. When combined with Ceftazidime, rel-Avibactam sodium exhibits significant inhibitory effects on Enterobacteriaceae producing Ambler class A and C β-lactamases. Its IC50 values are significantly lower than those of commonly used β-lactamase inhibitors like Clavulanic acid and Ticarcillin, demonstrating high efficacy against TEM-1 and P99 enzymes.

Piperacillin mixture with tazobactam (8:1) is a combination antibiotic known as Piperacillin-Tazobactam, formulated at an 8:1 ratio. This β-lactam/β-lactamase inhibitor duo exhibits broad-spectrum antibacterial activity, effective against a wide range of Gram-positive, Gram-negative aerobic, and anaerobic bacteria, including many pathogens that produce β-lactamase.

β-Lactamase-IN-2 is an inhibitor of β-Lactamase with anti-microbial and anti-bacterial effects.

β-Lactamase-IN-4 (WO2013149121A1, compound 708) is a potent β-lactamase inhibitor. It serves as a valuable tool in the investigation of bacterial infections.

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