βlactamase

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

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.

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

Metallo-β-lactamase-IN-13 (Compound 13i) serves as a pan Metallo-β-Lactamase inhibitor with extended activity against Gram-negative (GN) bacteria expressing metallo-β-lactamases. It exhibits antibacterial properties effective against P. aeruginosa [1].

Metallo-β-lactamase-IN-14 (Compound 17e) serves as an inhibitor of Metallo-β-Lactamase, displaying inhibitory activity against VIM-1 and VIM-2. This compound also exhibits antibacterial effects on Gram-negative (GN) bacteria and P. aeruginosa [1].

β-Lactamase-IN-6 is a β-lactamase inhibitor with high antibacterial activity.

β-Lactamase-IN-8 (compound 20) is a potent, orally bioavailable, broad-spectrum cyclic boronate β-lactamase inhibitor for antibacterial research [1].

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

Metallo-β-lactamase-IN-4 (compound 40) is a potent metallo-β-lactamase (MBL) inhibitor with IC50 values of 0.1 μM for VIM-1, 1.3 μM for NDM-1, and 5.0 μM for IMP-7, respectively [1].

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].

Metallo-β-lactamase-IN-15 (Compound ±13), a potent inhibitor of MBL, demonstrates IC 50 values of 0.29 μM for NDM-1, 0.088 μM for IMP-1, and 0.063 μM for VIM-2, respectively [1].

Metallo-β-lactamase-IN-4 (compound 40) is a potent inhibitor of metallo-β-lactamases (MBL) with IC50 values of 0.5 μM for VIM-1, 2.1 μM for NDM-1, and 3.3 μM for IMP-7, respectively [1].

Metallo-β-lactamase-IN-8 (compound 17) is a potent, reversible, and competitive broad-spectrum metallo-β-lactamases (MβLs) inhibitor with antibacterial activity, exhibiting IC50 values of 1.3 μM against L1, 5.7 μM against ImiS, 9.8 μM against IMP-1, and 9.9 μM against VIM-2 [1].

β-Lactamase-IN-7 (compound 14) is a potent inhibitor of VIM-type metallo-β-lactamase, effectively inhibiting Klebsiella pneumoniae with Ki values of 1.26 μM for VIM-1 and 0.54 μM for VIM-4 [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].

Metallo-β-lactamase-IN-9 (Compound 23) is a broad-spectrum inhibitor of metallo-beta-lactamases (MBL), with inhibition constants (IC50) of 35 nM for NDM-1, 269 nM for VIM-1, and 369 nM for IMP-1 [1].

Metallo-β-lactamase-IN-11 (compound 5f), a potent inhibitor of Metallo-β-lactamases (MBLs), demonstrates efficacy against bacterial metallophyllactamase CphA with an IC50 value of 45 µM. At 10 µM, it inhibits NDM-1 by 49% and AIM-1 by 61%, indicating its potential for research on countering antibiotic resistance [1].

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.

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-3 (compound 35) is a potent metallo-β-lactamases (MBL) inhibitor that can potentially restore the activity of current β-lactam antibiotics and provide an orthogonal strategy for discovering new antibiotics. It exhibits high activity against VIM-1 and NDM-1, with IC50 values of 0.6 and 1.0 μM, respectively, but does not inhibit IMP-7 [1].

β-LactaMase is a bacterially produced enzyme that hydrolyzes antibiotics such as penicillins, and its activity is inhibited by ethylenediaminetetraacetic acid (EDTA).