ndm-1 inhibitor-1

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

NDM-1 inhibitor-7 (Compound A8) is an NDM-1 inhibitor with an IC50 of 10.284 μM. It restores the ability of meropenem (MEM) to penetrate the cell wall of Gram-negative bacteria and effectively reinstates MEM's antibacterial activity against NDM-1 positive Escherichia coli. Moreover, NDM-1 inhibitor-7 demonstrates significant efficacy in both Galleria mellonella and murine peritonitis infection models.

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.

NDM-1 Inhibitor-5 (compound 57) exhibits strong inhibition of NDM-1, characterized by a K i of 2.5 μM. Additionally, it demonstrates synergistic antibacterial effects when combined with meropenem [1].

NDM-1 inhibitor-2 is an inhibitor of new delhi metallo-β-lactamase-1 (NDM-1).

NDM-1 Inhibitor-4 (compound 27) is an antimicrobial agent that inhibits NDM-1 with a K_i of 1.7 μM [1].

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.

Captopril (SA333) is a potent and specific inhibitor of peptidyl-dipeptidase A. It blocks the conversion of angiotensin I to angiotensin II, a vasoconstrictor and important regulator of arterial blood pressure.

TNF-α-IN-9 is an NDM-1 inhibitor-3 analog and is a TNF-α inhibitor.TNF-α-IN-9 shows low inhibitory activity.

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

Dacisteine (N,S-Diacetyl-L-cysteine) is an inhibitor of New Delhi metallo-beta-lactamase-1 (NDM-1) with an IC50 of 1000 μM.

YJ182 is an NDM-1 inhibitor with an IC50 of 0.23 μM, and additionally inhibits IMP-1, VIM-2, GIM-1, and MMP-2 with respective IC50 values of 0.25, 0.61, 0.49, and 6.92 μM. It is utilized in bacterial infection research [1].

SA09-Cu is a potent, noncompetitive inhibitor of NDM-1, with an IC50 of 9.6 nM. It inactivates NDM-1 by oxidizing the enzyme's Zn(II)-thiolate site and resists reduction by bacterial intracellular thiols. SA09-Cu effectively restores Meropenem efficacy against various clinical NDM-1-producing carbapenem-resistant Enterobacteriaceae (CRE) and hampers the progression of carbapenem resistance [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.

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-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.

MBL-IN-3 (compound 72922413), a potent inhibitor of New Delhi metallo-β-lactamase-1 (NDM-1) with an IC50 value of 54±4 μM, effectively reduces the minimum inhibitory concentrations (MICs) of Meropenem against clinical isolates of E. coli and K. pneumoniae that express NDM-1. This compound is utilized in studies focused on antibiotic sensitizer research [1].

Metallo-β-lactamase-IN-9 (Compound 23) is a broad-spectrum inhibitor of metallo-beta-lactamases (MBL), with inhibition constants (IC50) of 35 nM for NDM-1, 269 nM for VIM-1, and 369 nM for IMP-1 [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].

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].

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-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].

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.

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