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β-lactamase inhibitor
Avibactam is a covalent, reversible, non-β-lactam β-lactamase inhibitor.- Marta Gómara-Lomero, .et al. , Sci Rep, 2023, Sep 2;13(1):14429 PMID: 37660210
- Lara Muñoz-Muñoz, .et al. , Antibiotics (Basel), 2023, Feb; 12(2): 335 PMID: 36830246
- Moonsuk Bae, .et al. , Antibiotics (Basel), 2021, Dec 5;10(12):1492 PMID: 34943704
- Taeeun Kim, .et al. , Antibiotics (Basel), 2020, Dec 15;9(12):912 PMID: 33334045
- Annelien Everaert, .et al. , Antimicrob Resist Infect Control, 2016, 5: 44 PMID: 27895902
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β-lactamase inhibitor
Sulbactam is a beta-lactamase inhibitor with an average IC50 of 0.8 μM.- Pholwat S, .et al. , PLoS One, 2019, May 10;14(5):e0216747 PMID: 31075137
- Clavulanic acid is a mechanism-based β-lactamase inhibitorcombined with penicillin group antibiotics to overcome certain types of antibiotic resistance.
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beta-lactamase inhibitor
Durlobactam, also known as ETX2514, is a beta-lactamase inhibitor drug candidate. -
Cephalothin sodium is a semisynthetic, beta-lactam, first-generation cephalosporin antibiotic with bactericidal activity.
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non-β-lactam β-lactamase inhibitor
Avibactam sodium (NXL-104) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively. -
β-lactamase inhibitor
Zidebactam (WCK-5107) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL. -
non-β-lactam-β-lactamase inhibitor
Nacubactam (OP0595 free acid) is a potent non-β-lactam-β-lactamase inhibitor with activity against class A and class C β-lactamases. -
β-lactamase inhibitor
Taniborbactam is a potent inhibitor of β-lactamase, with IC50s of <100 nM for SHV-5, KPC-2, VIM-2, and AmpC β-lactamase, and 0.1 to 1 μM for OXA-1 β-lactamase, used in the research of bacterial infections. -
β-lactamase inhibitor
Vaborbactam is a cyclic boronic acid pharmacophore β-lactamase inhibitor. - beta-lactamase-IN-1 targets Neisseria gonorrhoeae infection which comprises administering to a subject in need thereof novel Tricyclic nitrogen containing compounds and corresponding pharmaceutical compositions as described herein.
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diazabicyclooctane inhibitor
Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases [ESBLs] and KPC) and class C (AmpC) enzymes. -
β-lactamase inhibitor
Zidebactam sodium salt (WCK-5107 sodium salt) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL. -
Antibiotic
Ceftazidime (GR20263), an antibiotic, has a broad spectrum activity against Gram-positive and Gram-negative aerobic bacteria. Ceftazidime is also active against Enterobacteriaceae (including β-lactamase-positive strains) and is resistant to hydrolysis by most β-lactamases. -
β-lactamase Inhibitor
Kalafungin is a β-lactamase inhibitor derived from marine Streptomyces, exhibiting an IC50 value of 225.37 μM. This compound demonstrates potent antimicrobial activity against a range of pathogenic fungi, yeasts, and protozoa, as well as significant effects on gram-positive bacteria like Staphylococcus aureus. Additionally, Kalafungin shows moderate activity against select gram-negative bacteria, making it a valuable tool for research in antibiotic resistance and microbial pathogenesis. -
β-lactamase Inhibitor
RDR 02308 is a β-lactamase inhibitor that targets the TLR4-MyD88 signaling pathway. This compound effectively inhibits the activity of full-length β-lactamase, providing a valuable tool for studies related to antibiotic resistance. Its mechanism of action makes it suitable for research applications focused on bacterial infections and the development of novel therapeutic strategies. -
β-lactamase Inhibitor
FPI-1523 is a potent β-lactamase inhibitor targeting CTX-M-15 and OXA-48, exhibiting dissociation constants (Kd) of 4 nM and 34 nM, respectively. Additionally, it inhibits penicillin-binding protein 2 (PBP2) with an IC50 of 3.2 μM. FPI-1523 demonstrates significant antimicrobial activity, making it a valuable reagent for research in antibiotic resistance and bacterial infection studies. -
Beta-lactamase Inhibitor
BLI-489 is a potent beta-lactamase inhibitor that effectively targets class A, class C (AmpC), and class D beta-lactamase producing pathogens. When used in combination with Piperacillin, BLI-489 enhances antimicrobial activity, providing a therapeutic strategy against infections caused by resistant bacteria. This compound is essential for research aimed at understanding and overcoming beta-lactam resistance mechanisms in clinical pathogens. -
Metallo-β-Lactamase Inhibitor
Thiomandelic acid is a potent inhibitor of metallo-β-lactamases, specifically targeting zinc-dependent enzymes. It exhibits broad-spectrum antibacterial activity by effectively preventing the hydrolysis of β-lactam antibiotics. This compound is valuable for research applications focused on antibiotic resistance mechanisms and the development of novel therapeutics against resistant bacterial infections. -
β-lactamase Inhibitor
Xeruborbactam bis-acetoxy methyl ester is a boronic acid derivative that functions as a β-lactamase inhibitor. This compound effectively targets β-lactamase enzymes, providing a mechanism to counteract antibiotic resistance in bacterial strains. It is primarily utilized in research focused on developing novel antibacterial therapies and studying the mechanisms of β-lactamase-mediated resistance. -
Metallo-β-lactamase Inhibitor
Metallo-β-lactamase-IN-16 is a potent metallo-β-lactamase inhibitor targeting critical enzymes responsible for antibiotic resistance. This sulfone-containing compound shows significant antibacterial activity by effectively inhibiting NDM-1, IMP-1, VIM-1, and VIM-2, with IC50 values of 0.16 nM, 0.23 nM, 0.31 nM, and 1.0 nM, respectively. It serves as a valuable tool for research in combating bacterial infections and understanding the mechanisms of antibiotic resistance. -
Metallo-β-Lactamase Inhibitor
EBL-3183 is a potent inhibitor of metallo-β-lactamases (MBLs) that targets the NDM-1 enzyme. This indole-2-carboxylate compound exhibits reversible, non-covalent, and competitive inhibition characterized by a pIC50 value of 7.7. EBL-3183 is valuable for research applications focused on combating antibiotic resistance and exploring mechanisms of MBL inhibition. -
β-lactamase Inhibitor
Xeruborbactam methoxy acetoxy methyl ester is a boronic acid derivative specifically designed as a β-lactamase inhibitor. This compound effectively inhibits the enzymatic activity of β-lactamases, which are responsible for antibiotic resistance in various bacterial strains. It is primarily utilized in research applications aimed at understanding β-lactamase mechanisms and developing novel antimicrobial therapies. -
β-lactamase Inhibitor
Pralurbactam is a potent β-lactamase inhibitor that enhances the antibacterial efficacy of Imipenem against Mycobacterium abscessus. Its ability to reduce pulmonary bacterial load in neutropenic mice highlights its potential as a significant therapeutic agent. This compound is valuable in research focused on infections caused by Mycobacterium abscessus complex, as well as strains of Escherichia coli and Klebsiella pneumoniae. -
β-lactamase Inhibitor
rel-Avibactam sodium is a potent β-lactamase inhibitor designed to combat bacterial resistance. It demonstrates broad-spectrum antibacterial activity, particularly against Enterobacteriaceae that produce Ambler A and C types of β-lactamases. When used in combination with Cefazidime, rel-Avibactam sodium exhibits significant inhibitory effects and offers enhanced efficiency compared to traditional β-lactamase inhibitors, as indicated by its low IC50 values against TEM-1 and P99 enzymes. This compound is essential for research into antibiotic resistance and the development of novel antibacterial therapies. -
β-lactamase Antibiotic
Tigemonam is a monobactam antibiotic that targets β-lactamase enzymes, demonstrating a Ki of 0.86 μM against Enterobacter cloacae P99 and 50.8 μM against Escherichia coli TEM-1. It binds to penicillin-binding proteins 1a, 3, and 4, effectively inhibiting bacterial cell wall synthesis and exhibiting bactericidal activity against a range of aerobic gram-negative bacteria, including Enterobacteriaceae, Haemophilus influenzae, and Neisseria gonorrhoeae. Tigemonam is resistant to hydrolysis by multiple β-lactamases and has been shown to reduce bacterial load in systemic and localized infections in rodent models. This compound is valuable for research into gram-negative bacterial infections, particularly acute pyelonephritis, lung infections, and thigh muscle infections. -
β-lactamase Inhibitor
Taniborbactam hydrochloride is a reversible and selective β-lactamase inhibitor that targets various β-lactamase enzymes, demonstrating IC50 values ranging from 8 to 530 nM, with specific IC50s of 30 nM for KPC-2, 32 nM for AmpC, 42 nM for OXA-48, and 20 nM for VIM-2. This compound is effective against Gram-negative bacteria, making it a valuable tool in the study of antibiotic resistance mechanisms and the development of novel antibacterial strategies. Researchers can utilize Taniborbactam hydrochloride in investigations aimed at enhancing the efficacy of β-lactam antibiotics. -
Beta-lactamase Inhibitor
Xeruborbactam disodium is a potent beta-lactamase inhibitor that targets both serine and metallo beta-lactamases with exceptional efficacy. This ultra-broad-spectrum compound operates at nanomolar concentrations, rendering it a valuable tool in combating antibiotic resistance. It is suitable for research applications aimed at understanding beta-lactamase mechanisms and developing new therapeutic strategies against resistant bacterial strains. -
Serine β-Lactamase Inhibitor
Pilabactam sodium is a potent serine β-lactamase inhibitor that demonstrates broad-spectrum activity, exhibiting IC50 values between 1 nM and 175 nM across various serine β-lactamase enzymes. This compound enhances the efficacy of β-lactam antibiotics against strains of Carbapenem-Resistant Enterobacterales (CRE) and Acinetobacter baumannii (CRAB). Pilabactam sodium is essential for research aimed at understanding and overcoming bacterial infections, particularly those caused by resistant pathogens. -
TEM-1 β-Lactamase Inhibitor
Cymal-6 (Cyclohexyl-hexyl-β-D-maltoside) is a potent inhibitor of TEM-1 β-lactamase, exhibiting a Ki value of 40.05 µM. This compound serves as a glycosidic surfactant, facilitating various biochemical applications. Its inhibitory properties make it valuable for research focused on antibiotic resistance and enzyme activity modulation. -
Beta-Lactamase Inhibitor
Ledaborbactam is a β-lactamase inhibitor that targets various β-lactamase enzymes, enhancing the efficacy of β-lactam antibiotics against resistant bacterial strains. This compound is instrumental in research focused on combating bacterial infections, especially those caused by multidrug-resistant organisms. Its ability to inhibit β-lactamases makes it a valuable tool for investigating and developing novel therapeutic approaches in infectious disease treatment. -
β-lactamase Inhibitor
Funobactam is a β-lactamase inhibitor that targets bacterial enzymes responsible for antibiotic resistance. This compound exhibits potent activity against various β-lactamases, making it a valuable tool in the study of antibiotic mechanisms and the development of novel antimicrobial agents. Funobactam is particularly useful in research applications focused on overcoming bacterial resistance to β-lactam antibiotics. -
Metallo-β-lactamase Inhibitor
MK-3402 is a potent metallo-β-lactamase inhibitor that exhibits IC50 values of 0.53 nM, 0.25 nM, and 0.169 nM against enzymes IMP-1, NDM-1, and VIM-1, respectively. This compound enhances the efficacy of beta-lactam antibiotics and is valuable in bacterial research, particularly in studies focused on combating antibiotic resistance. MK-3402's strong inhibitory properties make it a critical tool for investigating metallo-β-lactamase-mediated resistance mechanisms. -
Penem β-Lactamase Inhibitor
BLI-489 hydrate is a penem β-lactamase inhibitor that effectively targets class A, class C, and certain class D β-lactamases. This compound demonstrates notable biological activity when used in combination with Piperacillin, showing efficacy against murine infections caused by pathogens expressing extended-spectrum β-lactamases, AmpC β-lactamases, and class D β-lactamases. BLI-489 hydrate is a valuable reagent for research into antibiotic resistance and the development of combination therapies. -
β-lactamase Inhibitor
WCK-4234 is a potent β-lactamase inhibitor that effectively targets class A, C, and D β-lactamases. While lacking direct antibacterial activity, WCK-4234 enhances the efficacy of carbapenems such as imipenem and meropenem against Enterobacteriaceae possessing OXA-48/OXA-181 or KPC enzymes, as well as those exhibiting combinations of impermeability and AmpC or ESBL activity. This compound is particularly noteworthy for its ability to overcome resistance conferred by OXA-type carbapenemases, making it valuable for research in antibiotic resistance mechanisms. -
β-lactamase Inhibitor
FPI-1523 sodium is a potent β-lactamase inhibitor targeting CTX-M-15 and OXA-48, with dissociation constants (Kd) of 4 nM and 34 nM, respectively. Additionally, it inhibits penicillin-binding protein 2 (PBP2) with an IC50 of 3.2 μM. FPI-1523 sodium demonstrates significant antimicrobial activity, making it a valuable reagent in the study of antibiotic resistance and the development of novel antimicrobial therapies. -
β-Lactamase Inhibitor
Metallo β-lactamase ligand 1 is an established class B β-lactamase inhibitor that targets metallo-β-lactamases, enzymes responsible for antibiotic resistance. This compound exhibits significant antibacterial activity, making it a useful tool in combating infections caused by β-lactamase-producing bacteria. It is particularly valuable in research focused on developing new antimicrobial strategies and understanding the mechanism of β-lactamase-mediated resistance. -
β-lactamase Inhibitor
Brobactam sodium is a potent synthetic β-lactamase inhibitor that effectively targets various β-lactamase enzymes. This compound exhibits broad-spectrum antibacterial activity, making it a valuable tool for enhancing the efficacy of β-lactam antibiotics. Brobactam sodium is primarily utilized in research applications aimed at understanding antibiotic resistance mechanisms and developing new therapeutic strategies against resistant bacterial strains. -
Beta-lactamase Antibiotic
Ritipenem acoxil is an oral-active beta-lactamase antibiotic designed to inhibit bacterial cell wall synthesis. It demonstrates significant activity against various bacterial strains, making it a valuable tool in the study of bacterial pneumonia. This compound serves as a critical reagent for researchers investigating antibiotic resistance and the mechanisms of bacterial infections. -
β-lactamase Inhibitor
AM-112 is a potent β-lactamase inhibitor that targets class A, C, and D β-lactamase enzymes, demonstrating IC50 values as low as 0.0002 μg/mL. Its mechanism involves the inhibition of PBP2, a penicillin-binding protein in E. coli, thereby protecting Ceftazidime from enzymatic hydrolysis and enhancing its antibacterial activity against Gram-negative bacteria, enterococci, and staphylococci. AM-112 exhibits favorable pharmacokinetic properties and acid-base stability, making it a valuable tool for research into bacterial infections. -
β-lactamase Substrate
Nitrocefin is a chromogenic substrate specifically targeting β-lactamase enzymes. It displays a characteristic color shift from yellow to red upon hydrolysis of the β-lactam ring, enabling visual quantification of β-lactamase activity. This reagent is widely utilized in studies of enzyme inhibition and the development of β-lactamase-resistant antibiotics. -
Beta-lactamase Inhibitor
Avibactam sodium hydrate is a reversible non-β-lactam β-lactamase inhibitor that specifically targets β-lactamase enzymes TEM-1 and CTX-M-15, demonstrating IC50 values of 8 nM and 5 nM, respectively. This compound is crucial for enhancing the efficacy of β-lactam antibiotics against resistant bacterial strains. Its use in research applications includes investigations into antibiotic resistance mechanisms and the development of combination therapies to overcome β-lactamase-mediated resistance. -
β-lactamase Inhibitor
Clavulanate potassium is a potent β-lactamase inhibitor that enhances the effectiveness of β-lactam antibiotics by inhibiting bacterial enzyme activity. It is primarily used in research to study antimicrobial resistance mechanisms and to evaluate the synergy of antibiotic combinations. Clavulanate potassium is essential in elucidating bacterial adaptations and informing therapeutic strategies against resistant organisms. -
β-lactamase Inhibitor
Clavulanate lithium is a potent β-lactamase inhibitor that enhances the efficacy of β-lactam antibiotics by inhibiting bacterial enzymes responsible for antibiotic resistance. Its ability to combat antibiotic resistance makes it invaluable in research focused on understanding and overcoming treatment failures caused by resistant pathogens. Clavulanate lithium is commonly used in studies investigating the mechanisms of resistance and in the development of novel therapeutics. -
β-lactamase Inhibitor
Sulbactam pivoxil is a prodrug of Sulbactam, functioning primarily as a β-lactamase inhibitor. It demonstrates significant antibacterial activity by overcoming resistance mechanisms associated with β-lactam antibiotics. This compound is characterized by enhanced absorption compared to Sulbactam, leading to elevated serum concentrations following oral administration, making it a valuable tool for research on antibiotic resistance and evaluation of combination therapies. -
β-lactamases
Cephalosporinase, bacillus is an enzyme that functions as a β-lactamase, inactivating and degrading the activity of cephalosporin antibiotics. This enzyme is essential for research on antibiotic resistance mechanisms in bacteria, as it allows the study of the efficacy of cephalosporins against resistant strains. It is useful in developing strategies to combat bacterial infections and improve antibiotic therapies.

