β-lactamase-in-2

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-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].

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

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.

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.

KPC-IN-1 (compound 1e) is an inhibitor of Klebsiella pneumoniae carbapenemase KPC-2, with an IC50 value of 8.3 nM. KPC is a β-lactamase expressed in Gram-negative bacteria that hydrolyzes carbapenems, leading to significant bacterial resistance to carbapenem antibiotics.

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)

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.

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].

Captopril (SQ 14225) hydrochloride is an antihypertensive agent that is a thiol-containing, competitive, orally active angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 0.025 μM, widely used in hypertension and congestive heart failure research. It is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM [1] [2] [3].

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-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].

VIM-2-IN-1 (compound 1dj) is a β-lactamase inhibitor with antibacterial activity, demonstrating an IC50 of 48 μM, and inhibits New Delhi Metal (NDM-1) with an IC50 of 231 μM.

Cefcanel is a semisynthetic third-generation cephalosporin with antibacterial activity. Cefcanel is active against the species E. coli, K. aerogenes and Proteus mirabilis; H. influenzae and M. catarrhalis has reasonable susceptibility. Cefcanel inhibits 90% of S. aureus strains at 2 µg ml, irrespective of the presence of a β-lactamase. Cefcanel binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.

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

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].

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].