β-lactamase inhibitor

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

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.

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.

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.

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.

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

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.

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.

(+)-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.

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

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

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

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.

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

Cloxacillin sodium monohydrate (Cloxacillin Sodium) is the sodium salt of cloxaclliin, a semisynthetic beta-lactamase resistant penicillin antibiotic with antibacterial activity.

FPI-1523, a derivative of Avibactam, is a potent inhibitor of β-lactamase enzymes. It has Kd values of 4 nM and 34 nM for CTX-M-15 and OXA-48, respectively. Additionally, FPI-1523 inhibits PBP2 with an IC50 of 3.2 μM and demonstrates significant antimicrobial activity.

Clavicoronic acid is a β-lactam drug that functions as a mechanism-based β-lactamase inhibitor. While not effective by itself as an antibiotic, when combined with penicillin-group antibiotics, it can overcome antibiotic resistance in bacteria that secrete β-lactamase, which otherwise inactivates most penicillins.

RDR 02308 is a TLR4-MyD88 binding inhibitor that inhibits full-length β-lactamase [1] .

FPI-1602 is a β-lactamase inhibitor with strong antimicrobial activity against Pseudomonas aeruginosa, Escherichia coli, and Enterobacter species [1].

Cefuroxime Sodium is the sodium salt form of cefuroxime and a semi-synthetic, broad-spectrum, beta-lactamase resistant, second-generation cephalosporin antibiotic with bactericidal activity. Cefuroxime sodium (Cefuroxime sodium salt) inhibits bacterial cell wall synthesis by inactivating penicillin binding proteins (PBPs) thereby interfering with the final transpeptidation step required for cross-linking of peptidoglycan units which are a component of the cell wall. Lack of cross-linking results in a reduction of cell wall stability and leads to cell lysis.

Nacubactam (OP0595 free acid) is a potent inhibitor of non-β-lactam-β-lactamase with activity against class A and class C β-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.

NDM-1 inhibitor-1 is an inhibitor of new delhi metallo-β-lactamase-1 (NDM-1).

ANT3310 is an inhibitor of broad-spectrum covalent Serine β-Lactamase with IC50s ranging from 1 nM to 175 nM for AmpC, CTX-M-15, TEM-1, OXA-48, OXA-23, and KPC-2. ANT3310 can be used in studies about bacterial infection.

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

Taniborbactam is a reversible and selective boronic acid-containing pan-spectrum β-lactamase inhibitor (IC50s: 8-530 nM). Taniborbactam has IC50s of 30 nM, 32 nM, 42 nM, 20 nM for KPC-2, AmpC, OXA-48, and VIM-2.

Captopril (SQ 14225) hydrochloride is an antihypertensive agent that is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor with IC 50 of 0.025 μM and has been widely used for research of hypertension and congestive heart failure. Captopril hydrochloride is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC 50 of 7.9 μM [1] [2] [3].

Avibactam sodium hydrate (NXL-104 hydrate) is a covalent and reversible inhibitor of β-lactamase that does not contain a β-lactam core. Avibactam sodium hydrate inhibits β-lactamase CTX-M-15 and TEM-1 with IC 50 s of 5 nM and 8 nM, respectively.

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].

FPI-1465 is a dual inhibitor of serine-β-Lactamases and Penicillin-binding proteins (PBPs), demonstrating inhibition of PBP2 with an IC50 of 1.0 μg/mL. Additionally, it exhibits activity against β-lactamase CTX-M-15 and OXA-48, with dissociation constants (Kd) of 0.011 μM and 5.3 μM, respectively [1].

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].

Nafcillin sodium, an antibiotic, acts as a reversible inhibitor of β-lactamase, making it effective for research into staphylococcal infections [1] [2].

VNRX-5133 is an injectable broad-spectrum β-lactamase inhibitor. VNRX-5133 is a novel β-lactamase inhibitor with potent and selective direct inhibitory activity against both serines- and Metallo-β-lactamases.

QPX7728 methoxy acetoxy methy ester is an inhibitor of boronic acid β-lactamase.

Funobactam is a potent β-lactamase inhibitor.

Thiomandelic acid is a simple, broad-spectrum and quite potent metallo-β-lactamase inhibitor, an antimicrobial compound.

FPI-1523 sodium, a derivative of avibactam, is a potent β-lactamase inhibitor with K d s of 4 nM and 34 nM for CTX-M-15 and OXA-48, respectively.FPI-1523 sodium inhibited PBP2 with an IC 50 of 3.2 μM.FPI-1523 sodium has a high level of antibacterial activity. FPI-1523 sodium has considerable antimicrobial activity.

MBL-IN-1 (compound 41), a β-Lactamase inhibitor, exhibits an IC50 range of 0.10 to 25.85 µM and is utilized in the study of bacterial infections [1].

Sulbactam (CP45899) is a semi-synthetic beta-lactamase inhibitor. The beta-lactam ring of sulbactam irreversibly binds to beta-lactamase at or near its active site, thereby blocking enzyme activity and preventing metabolism of other beta-lactam antibiotics by the enzyme. Combining this agent with a beta-lactamase susceptible antibiotic, such as penicillins or a cephalosporin, to treat infections caused by beta-lactamase producing organisms, results in a decreased turnover rate of the beta-lactamase sensitive antibiotic and enhances its antibacterial activity.

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].

O-Benzylhydroxylamine is a building block.1,2It has been used in the synthesis of β-lactam inhibitor precursors and fluoroquinolone derivatives with antibiotic activity. 1.Bellettini, J.R., and Miller, M.J.A short synthesis of an important precursor to a new class of bicyclic β-lactamase inhibitorsTetrahedron Lett.38(2)167-168(1997) 2.Asadipour, A., Moshafi, M.H., Khosravani, L., et al.N-substituted piperazinyl sarafloxacin derivatives: synthesis and in vitro antibacterial evaluationDaru.26(2)199-207(2018)

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

Thiamphenicol (Dextrosulphenidol) is a methylsulfonyl analog of chloramphenicol. It is an antibiotic and immunosuppressive agent.