ndm 1 inhibitor 1

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

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

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-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].

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.

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

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

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.

epi-D-Captopril (epi-D-SQ 14225) is a stereoisomer of Captopril and functions as an inhibitor of metallo-beta-lactamases (MBLs). The IC50 values of epi-D-Captopril for NDM-1, IMP-1, and VIM-2 are 64 μM, 173 μM, and 5.5 μM, respectively. This compound holds potential for research in MBLs-related antibiotic-resistant infections.

MBL-IN-5 is an inhibitor of metallo-β-lactamase (MBL). It effectively suppresses three clinically significant B1 subfamily MBLs: NDM-1, VIM-1, and IMP-1 with IC50 values of 0.05 nM, 14 nM, and 21 nM respectively. MBL-IN-5 notably enhances the efficacy of carbapenem antibiotics against MBL-producing clinical strains and, when combined with IPM antibiotics, significantly reduces bacterial load in a thigh infection model.

Metallo-β-lactamase-IN-12 is a dual inhibitor targeting Metallo-β-lactamase [MβLs (NDM-1, IMP-1)] and Serine β-lactamase [SβLs (OXA-48, KPC-2)], displaying IC50 values of 0.64 μM, 1.32 μM, 1.01 μM, and 0.57 μM respectively. Metallo-β-lactamase-IN-12 also exhibits antibacterial activity.

MBL-IN-2 ((2R, 2R')-5αC) is a Metallo-β-lactamase (MBL) inhibitor that effectively inhibits New Delhi Metallo-β-lactamase-1 (NDM-1) with an IC50 of 0.3 μM. MBL-IN-2 ((2R, 2R')-5αC) can be used in research on resistance to β-lactam antibiotics.

MBL-IN-4 (compound 4b) is an MBL inhibitor with IC50 values of 4.81 μM for IMP-1 and 33 μM for NDM-1.

ANT2681 is a potent NDM inhibitor with a Ki value of 0.04 μM for NDM-1. It also inhibits other MBLs such as VIM-1 and IMP-1, with Ki values of 0.63 μM and 3.81 μM, respectively. ANT2681 can be used in combination with Meropenem to suppress infections caused by NDM-producing Enterobacteriaceae.

NDM-1-IN-9 (compound M7) is an orally active NDM-1 inhibitor with a Ki value of 3.95 nM.

MBL-IN-6 (Compound 6d) is a metal-β-lactamase (MBL) inhibitor with Ki values of 2.6 μM for NDM-1 and 0.08 μM for VIM-2. It acts synergistically with Imipenem against clinical isolates producing MBL, such as E. coli SI-M001, K. pneumoniae T2301, and S. marcescens SI-1591, with a MIC ranging from 2-64 μg/mL. MBL-IN-6 does not induce off-target effects and exhibits no inhibitory activity against ACE-1. This compound is useful for research on antibiotic resistance.

NDM-1-IN-10 (Compound CS-23) is an irreversible covalent inhibitor of New Delhi metallo-β-lactamase-1 (NDM-1) with an IC50 of 36 nM. It displays synergistic effects with Meropenem against E. coli expressing NDM-1, with a minimum inhibitory concentration (MIC) of 0.25 μg/mL for E. coli BL21/pET15b-blaNDM-1. NDM-1-IN-10 is applicable in bacterial infection research.

NDM-1-IN-11 is a potent covalent inhibitor of NDM-1 with an IC50 of 1.12 μM, acting by forming a Se-S bond with the enzyme. In both in vivo and in vitro models, NDM-1-IN-11, when combined with Meropenem, effectively inhibits the growth of NDM-1-producing E. coli. This compound is suitable for research addressing bacterial resistance caused by NDM-1.

NDM-1-IN-12 (Compound 10c) is an inhibitor of NDM-1 metallo-β-lactamase, exhibiting an IC50 value of 9 nM. It effectively reverses bacterial resistance to β-lactam antibiotics and shows a synergistic effect when used in combination with antibiotics and SBL inhibitors. NDM-1-IN-12 is utilized in research on combating multidrug-resistant bacteria.

Copper (II) pyrithione is an inhibitor of New Delhi metallo-β-lactamase 1 (NDM-1). It functions by transmetalation, substituting its zinc (II) cofactor with copper (II), and exhibits cytotoxic effects on pancreatic cancer cells and osteosarcoma cells. Additionally, Copper (II) pyrithione has antimicrobial properties against gram-positive bacteria and certain gram-negative bacteria. It can enhance the efficacy of β-lactam antibiotics against β-lactam-resistant bacteria synergistically. This compound can be utilized in research related to pancreatic cancer, osteosarcoma, and bacterial infections.

ATMpotentiator-1 (compound 9) acts as a β-lactamase inhibitor and efflux pump inhibitor with an IC50 of 1.6 μM for NDM-1, 12.5 μM and 5.4 μM for OXA-10, 5.0 μM for VIM-2, 26.7 μM for KPC-2, and 3.4 μM for OXA-48. It inhibits efflux pump activity in *Pseudomonas aeruginosa* and shows synergistic inhibitory effects when used with CCCP. ATMpotentiator-1 is applicable in research on carbapenem-resistant *Pseudomonas aeruginosa* (CRPA) infections.