β-lactamase-in-1

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.

Metallo-β-lactamase-IN-11 (compound 5f), a potent inhibitor of Metallo-β-lactamases (MBLs), demonstrates efficacy against bacterial metallophyllactamase CphA with an IC50 value of 45 µM. At 10 µM, it inhibits NDM-1 by 49% and AIM-1 by 61%, indicating its potential for research on countering antibiotic resistance [1].

Metallo-β-lactamase-IN-13 (Compound 13i) serves as a pan Metallo-β-Lactamase inhibitor with extended activity against Gram-negative (GN) bacteria expressing metallo-β-lactamases. It exhibits antibacterial properties effective against P. aeruginosa [1].

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].

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

NDM-1 inhibitor-8 (Compound 18b) is a covalent inhibitor of New Delhi metallo-β-lactamase-1 (NDM-1), with an IC50 of 7.03 μM. It effectively inhibits resistant bacterial strains and demonstrates synergistic antibacterial effects when used in combination with Meropenem. In mouse models, NDM-1 inhibitor-8 exhibits anti-infective activity.

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].

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].

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].

β-Lactamase-IN-8 (compound 20) is a potent, orally bioavailable, broad-spectrum cyclic boronate β-lactamase inhibitor for antibacterial research [1].

NDM-1 inhibitor-3 is a New Delhi Metallo-β-lactamase-1 (NDM-1) inhibitor (Ki : 4 μM) widely found in nature and is associated with antibiotic resistance.

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-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].

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

Metallo-β-lactamase-IN-5 (compound 5c) is a potent inhibitor of metallo-β-lactamases (MBLs), demonstrating inhibitory activity against MBLs NDM-1 and VIM-1. It effectively inhibits HUVECs with an IC50 value of 45 μg mL. Additionally, when combined with Imipenem, Metallo-β-lactamase-IN-5 exhibits synergistic antimicrobial activity [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.

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