lactamase

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

β-Lactamase-IN-6 is a β-Lactamase inhibitor that shows high antibacetrial activity.

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-8 (compound 20) is a potent and oral bioavailable broad-spectrum cyclic boronate β-lactamase inhibitor that can be used for researching antibacteria [1].

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

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

Metallo-β-lactamase-IN-4 (compound 40) is a potent metallo-β-lactamases (MBL) inhibitor with IC 50 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 powerful inhibitor of metallo-β-lactamases (MBLs). Its inhibitory activity against MBLs NDM-1 and VIM-1 has been demonstrated. With an IC50 value of 45 μg/mL, Metallo-β-lactamase-IN-5 effectively inhibits HUVECs. Additionally, when combined with Imipenem, Metallo-β-lactamase-IN-5 exhibits synergistic antimicrobial activity [1].

Metallo-β-lactamase-IN-4 (compound 40) is a potent inhibitor of metallo-β-lactamases (MBL) with IC 50 values of 0.5 μM, 2.1 μM, and 3.3 μM for VIM-1, NDM-1 and 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. The IC50 values of Metallo-β-lactamase-IN-8 against L1, ImiS, IMP-1 and VIM-2 are 1.3 μM, 5.7 μM, 9.8 μM, and 9.9 μM, respectively [1].

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

Metallo-β-lactamase-IN-7 is a potent inhibitor of VIM -Type metallo-β-lactamase with IC 50 s of 0.019 μM, 13.64 μM, 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 the Gram-negative bacterial strains [1].

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

Metallo-β-lactamase-IN-9 (Compound 23) serves as a broad-spectrum inhibitor of metallo-beta-lactamases (MBL), exhibiting 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 the bacterial metallophyllactamase CphA with an IC50 value of 45 µM. At a concentration of 10 µM, Metallo-β-lactamase-IN-11 inhibits NDM-1 by 49% and AIM-1 by 61%, indicating its potential application in research focused 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 IC 50 values of 0.56 μM, 29.50 μM, and 5.78 μM for VIM-2, VIM-1, and VIM-5, respectively. In addition, 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 has the potential to restore the activity of current β-lactam antibiotics and to offer an orthogonal strategy to the discovery of new antibiotics. Metallo-β-lactamase-IN-3 shows high activity against VIM-1 and NDM-1, with IC 50 of 0.6 and 1.0 μM, respectively. Metallo-β-lactamase-IN-3 does not show inhibition of IMP-7 [1].

Durlobactam sodium salt (ETX2514 sodium salt) is an inhibitor of β-lactamase with IC50 values of 4 nM, 14 nM, and 190 nM for Class A KPC-2, Class C AmpC, and Class D OXA-24, respectively. Durlobactam sodium salt can be used in studies about drug-resistant Gram-negative bacteria including Acinetobacter baumannii.

Avibactam sodium (NXL-104) is a reversible β-lactamase inhibitor (IC50: 8/80/38 nM, for TEM-1/P99/KPC-2 β-lactamases).

Cefditoren pivoxil (ME 1207) is a semi-synthetic, broad-spectrum, beta-lactamase resistant, third-generation cephalosporin antibiotic with bactericidal activity.

WCK-5153 is an enhancer of β-Lactamase and an inhibitor of PBP2 with antimicrobial activities against Pseudomonas aeruginosa. WCK-5153 can be used in studies about the treatment of serious infections caused by highly drug-resistant Gram-negative pathogens.

(3R,6R)-Vaborbactam ((3R,6R)-Vaborbactam (Iso-1360457-46-0)) is a cyclic boronic acid pharmacophore β-lactamase inhibitor with potential antimicrobial activity. (S)-Vamicamide ((S)-Vamicamide (Iso-132373-81-0)) is a novel anticholinergic compound.

Vaborbactam ammonium salt is a β-lactamase inhibitor that restores carbapenem activity against KPC-producing strains and is often used in conjunction with other drugs to study fungal infections.

Vaborbactam (RPX7009) is a β-lactamase inhibitor that is often used in conjunction with meropenem to study pneumonia and CRE infections.

Sulopenem, an orally active, potent inhibitor of beta-lactamase, is a parenteral penem antibiotic with broad-spectrum activities against Gram-negative and Gram-positive bacteria.

Taniborbactam dihydrochloride (VNRX-5133 dihydrochloride) is a selective and potent novel cyclic boronic acid β-lactamase inhibitor with antimicrobial activity and significant inhibition of Gram-negative bacteria.Taniborbactam dihydrochloride inhibits KPC Taniborbactam dihydrochloride inhibits KPC-2, AmpC, OXA-48 and VIM-2 and can be used for the study of fungal infections.

Durlobactam is a drug candidate for beta-lactamase inhibitor.

Durlobactam Triethylamine (ETX2514 Triethylamine) is a diazabicyclooctane β-lactamase inhibitor that inhibits classes A, C, and D β-lactams.Durlobactam Triethylamine has antifungal infection activity.

QPX7728 is an of ultra-broad-spectrum boronic acid beta-lactamase.

Cilastatin (MK0791) is a renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Since the antibiotic, IMIPENEM, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to increase its effectiveness. The drug also inhibits the metabolism of leukotriene D4 to leukotriene E4.

Nafcillin sodium monohydrate (CL 8491) is the sodium salt form of nafcillin, a semi-synthetic naphthalene, penicillin-related Nafcillin inhibits bacterial wall synthesis by a mechanism of action similar to penicillin. Penicillinase-resistant Nafcillin is used to treat infections caused by penicillin-resistant strains of Staphylococci.

Carbenicillin disodium (BRL-2064) is a broad-spectrum, semi-synthetic penicillin antibiotic with bactericidal and beta-lactamase resistant activity.

Piperacillin (Pipercillin) is a semisynthetic penicillin with wide spectrum of antimicrobial activity(particularly pseudomonas strains)

Iedaborbactam, as a beta-lactamase inhibitor (WO2015191907, Example 62), can be used for the research of bacterial infections.

IMB-XH1 (Mcl1-IN-2) is a myeloid cell factor 1 (Mcl-1) inhibitor.

Sultamicillin is an orally active double prodrug of Ampicillin/Sulbactan. Sulbactam is a semisynthetic β-Lactamase inhibitor.

(+)-Thienamycin, a powerful broad-spectrum antibacterial and β-lactamase inhibitor, is isolated from Streptomyces cattleya [1].

BLI-489 hydrate is a penicillin β-lactamase inhibitor that acts on classes A and C and some class D β-lactamases.

TINK-IN-1 is a selective and potent TNIK inhibitor (IC50: 8 nM).TINK-IN-1 inhibits colorectal cancer cell viability and can be used to study mental retardation.

Ledaborbactam etzadroxil (VNRX-7145) is an orally active inhibitor of Ambler class A, C, and D β-lactamase enzymes.

CENTA is a research center β - The color substrate of lactamase.

Penicillinase is a beta-lactamase. beta-lactamase enzymes inactivate beta-lactam antibiotics by hydrolyzing the peptide bond of the characteristic four-membered beta-lactam ring rendering the antibiotic ineffective [1] .

K-252c is a staurosporine analog isolated from Nocardiopsis sp. and is a cell-permeable PKC inhibitor (IC50: 2.45 μM). K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase. K-252c causes apoptosis in human chronic myelogenous leukemia cancer cells.

Zndm19 is an inhibitor of New Delhi Metallo-β-lactamase-1 (NDM-1), utilized in researching drug-resistant bacterial infections [1].

Cefmenoxime is a cephalosporin antibiotic administered intravenously or intramuscularly. It is an effective inhibitor of Enterobacteriaceae and is resistant to beta-lactamase-initiated hydrolysis. It is active against most common gram-positive and gram-ne

Dicloxacillin Sodium (BRL1702 Sodium) is a β-lactamase resistant penicillin similar to oxacillin and it has activity against gram-positive/negative aerobic and anaerobic bacteria.

Compound YJ196 (Compound 59) serves as an inhibitor of New Delhi Metallo-β-lactamase-1 (NDM-1) [1].

Avibactam sodium (NXL-104) dihydrate inhibits CTX-M-15 and β-lactamase TEM-1 with IC 50 s of 5 nM and 8 nM, respectively. Avibactam sodium dihydrate is a reversible and covalent inhibitor of non-β-lactam β-lactamase [1].

MßL-IN-2I is a potent broad-spectrum metallo-β-lactamase (MβL) inhibitor which inhibits the MβLs NDM-1, VIM-2, ImiS, and L1.