β-lactamases

Meropenem (SM 7338) is a broad-spectrum carbapenem antibiotic administered intravenously for severe bacterial infections caused by sensitive agents. It commonly causes mild, transient aminotransferase elevations and can rarely lead to clinically apparent cholestatic liver injury.

Relebactam (MK-7655) is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases.

Nitrocefin is an antibiotic. It being sensitive to hydrolysis by all lactamases produced by gram-positive and gram-negative bacteria.

Cefmenoxime hydrochloride (Cefmenoxime hemihydrochloride) is a cephalosporin antibiotic that is administered intravenously or intramuscularly. It is active against most common gram-positive and gram-negative microorganisms, is a potent inhibitor of Enterobacteriaceae, and is highly resistant to hydrolysis by beta-lactamases. The drug has a high rate of efficacy in many types of infection and to date, no severe side effects have been noted.

Meropenem trihydrate (SM 7338 trihydrate) is a carbapenem antibiotic with broad-spectrum antibacterial activity.

Avibactam Tetrabutylammonium is the salt form of Avibactam.Avibactam is a non-β-lactam β-lactamase inhibitor that inhibits TEM-1, P99, and KPC-2 β-lactamases (IC50=8 80 38 nM) with covalent and reversible and can be used to treat urinary tract infections.

Avibactam sodium (NXL-104) is a non-β-lactam β-lactamase inhibitor that inhibits TEM-1, P99, and KPC-2 β-lactamases (IC50=8 80 38 nM) covalently and reversibly. Avibactam sodium has antimicrobial activity and can be used to treat urinary tract infections.

QPX7728 disodium (Xeruborbactam disodium) is a cyclic boronate inhibitor of many serine and metal-β-lactamases with antibacterial activity, used in research on bacterial infections.

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

Nacubactam (OP0595 free acid) is a potent non-β-lactam β-lactamase inhibitor, effective against class A and class C β-lactamases.

Tazobactam (YTR-830H) is an antibacterial penicillin derivative which inhibits the action of bacterial beta-lactamases.

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.

LYS228 (also known as Ancremonam) is a potent antibiotic effective against carbapenem-resistant Enterobacteriaceae bacteria (MIC90 = 2 uM mL). It demonstrates strong antibacterial activity against CRE isolates even in the presence of all classes of β-lactamases.

WCK-4234 sodium (WCK 4234) is an inhibitor of β-lactamase can be used in studies targeting MDR infections. WCK-4234 sodium inhibits class A, C, and D β-lactamases and OXA carbapenemases.

Cephamycin C (CepC) is a nontoxic β-lactam antibiotic distinguished by its superior resistance to β-lactamases compared to other cephalosporins.

2-Aminoimidazole is a potent antimicrobial agent that effectively targets drug-resistant Mycobacterium tuberculosis by disrupting the proton motive force and blocking the electron transport chain, potentiates the action of beta-lactam antibiotics against Mycobacterium tuberculosis by decreasing the secretion of beta-lactamases and increasing the permeability of cell membranes, activates drug-resistant bacteria and improves therapeutic efficacy.

ARX-1796 (AV-006), an Avibactam prodrug, is an orally bioavailable β-lactamase inhibitor. Avibactam has a spectrum of inhibition of class A and C β-lactamases, including ESBLs, AmpC and Klebsiella pneumoniae carbapenemase (KPC) enzymes.

Ceftizoxime (Epocelin) is a cephalosporin-based, potent antibacterial agent which can be administered intravenously or by suppository. It is highly resistant to a broad spectrum of beta-lactamases and is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative organisms.

Ertapenem sodium (MK-826) is a new long-acting 1-β-methyl carbapenem antibiotic with a broad antibacterial spectrum including common aerobic and anaerobic bacteria and organisms with extended-spectrum β-lactamases.

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].

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-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].

Avibactam sodium hydrate (NXL-104 hydrate) is a highly effective β-lactamase inhibitor that inhibits β-lactamases TEM-1 and CTX-M-15, as well as the carbapenemase produced by Klebsiella pneumoniae and carbapenem-resistant Enterobacteriaceae.

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].