An updated patent review of metallo-β-lactamase inhibitors (2020–2023)

E Denakpo, T Naas, BI Iorga - Expert Opinion on Therapeutic …, 2023 - Taylor & Francis
ABSTRACT Introduction Metallo-β-lactamases (MBLs) are enzymes produced by bacteria
that confer resistance to most β-lactam antibiotics, including carbapenems, which have the …

[HTML][HTML] Recent developments to cope the antibacterial resistance via β-lactamase inhibition

Z Iqbal, J Sun, H Yang, J Ji, L He, L Zhai, J Ji, P Zhou… - Molecules, 2022 - mdpi.com
Antibacterial resistance towards the β-lactam (BL) drugs is now ubiquitous, and there is a
major global health concern associated with the emergence of new β-lactamases (BLAs) as …

Discovery of 2-Aminothiazole-4-carboxylic Acids as Broad-Spectrum Metallo-β-lactamase Inhibitors by Mimicking Carbapenem Hydrolysate Binding

YH Yan, TT Zhang, R Li, SY Wang, LL Wei… - Journal of Medicinal …, 2023 - ACS Publications
Metallo-β-lactamases (MBLs) are zinc-dependent enzymes capable of hydrolyzing all
bicyclic β-lactam antibiotics, posing a great threat to public health. However, there are …

1, 2, 4-Triazole-3-thione analogues with an arylakyl group at position 4 as metallo-β-lactamase inhibitors

L Gavara, F Verdirosa, L Sevaille, A Legru… - Bioorganic & medicinal …, 2022 - Elsevier
Abstract Metallo-β-lactamases (MBLs) represent an increasingly serious threat to public
health because of their increased prevalence worldwide in relevant opportunistic Gram …

[HTML][HTML] Fluorinated captopril analogues inhibit metallo-β-lactamases and facilitate structure determination of NDM-1 binding pose

A Kondratieva, K Palica, C Frøhlich, RR Hovd… - European Journal of …, 2024 - Elsevier
Bacterial resistance to the majority of clinically used β-lactam antibiotics is a global health
threat and, consequently, the driving force for the development of metallo-β-lactamase …

Discovery of hydroxamate as a promising scaffold dually inhibiting metallo-and serine-β-lactamases

XR Wu, WY Chen, L Liu, KW Yang - European Journal of Medicinal …, 2024 - Elsevier
The bacterial infection mediated by β-lactamases MβLs and SβLs has grown into an
emergent health threat, however, development of a molecule that dual inhibits both MβLs …

[HTML][HTML] A stepwise one-pot synthesis of aliphatic thiols and their derivatives from acrylamides and sulfur

AG Németh, R Szabó, K Németh, GM Keserű… - Organic & …, 2022 - pubs.rsc.org
Elemental sulfur enables the convenient formation of C–S bonds and the direct incoporation
of S–S bonds. The reactivity of easily accessible electron deficient alkenes towards sulfur …

[HTML][HTML] Drug Discovery in the Field of β-Lactams: An Academic Perspective

LMC Jacobs, P Consol, Y Chen - Antibiotics, 2024 - mdpi.com
β-Lactams are the most widely prescribed class of antibiotics that inhibit penicillin-binding
proteins (PBPs), particularly transpeptidases that function in peptidoglycan synthesis. A …

The crystal structure of the H116Q mutant of NDM-1: An enzyme devoid of zinc ions

WP Kong, YW Chen, KY Wong - Journal of Structural Biology, 2022 - Elsevier
New Delhi metallo-β-lactamase 1 (NDM-1) is an important causative factor of antimicrobial
resistance due to its efficient hydrolysis of a broad range of β-lactam compounds. The two …

Thiols as a privileged scaffold against metallo-β-lactamases

C Chen, D Wang, KW Yang - Privileged Scaffolds in Drug Discovery, 2023 - Elsevier
Gram-negative bacteria producing metallo-β-lactamases (MβLs), which hydrolyze almost all
β-lactams, including penicillins, cephalosporins, and carbapenems, are important …