4-Amino-1, 2, 4-triazole-3-thione-derived Schiff bases as metallo-β-lactamase inhibitors

L Gavara, L Sevaille, F De Luca, P Mercuri… - European Journal of …, 2020 - Elsevier
Resistance to β-lactam antibiotics in Gram-negatives producing metallo-β-lactamases
(MBLs) represents a major medical threat and there is an extremely urgent need to develop …

1, 2, 4‐Triazole‐3‐Thione Analogues with a 2‐Ethylbenzoic Acid at Position 4 as VIM‐type Metallo‐β‐Lactamase Inhibitors

F Verdirosa, L Gavara, L Sevaille, G Tassone… - …, 2022 - Wiley Online Library
Abstract Metallo‐β‐lactamases (MBLs) are increasingly involved as a major mechanism of
resistance to carbapenems in relevant opportunistic Gram‐negative pathogens …

4-(N-Alkyl- and -Acyl-amino)-1,2,4-triazole-3-thione Analogs as Metallo-β-Lactamase Inhibitors: Impact of 4-Linker on Potency and Spectrum of Inhibition

L Gavara, F Verdirosa, A Legru, PS Mercuri, L Nauton… - Biomolecules, 2020 - mdpi.com
To fight the increasingly worrying bacterial resistance to antibiotics, the discovery and
development of new therapeutics is urgently needed. Here, we report on a new series of 1 …

1, 2, 4-Triazole-3-thione compounds with a 4-ethyl alkyl/aryl sulfide substituent are broad-spectrum metallo-β-lactamase inhibitors with re-sensitization activity

A Legru, F Verdirosa, JF Hernandez, G Tassone… - European Journal of …, 2021 - Elsevier
Abstract Metallo-β-lactamases (MBLs) are important contributors of Gram-negative bacteria
resistance to β-lactam antibiotics. MBLs are highly worrying because of their …

Optimization of 1, 2, 4-triazole-3-thiones toward broad-spectrum metallo-β-lactamase inhibitors showing potent synergistic activity on VIM-and NDM-1-producing …

A Legru, F Verdirosa, Y Vo-Hoang… - Journal of Medicinal …, 2022 - ACS Publications
Metallo-β-lactamases (MBLs) contribute to the resistance of Gram-negative bacteria to
carbapenems, last-resort antibiotics at hospital, and MBL inhibitors are urgently needed to …

4-Alkyl-1, 2, 4-triazole-3-thione analogues as metallo-β-lactamase inhibitors

L Gavara, A Legru, F Verdirosa, L Sevaille, L Nauton… - Bioorganic …, 2021 - Elsevier
In Gram-negative bacteria, the major mechanism of resistance to β-lactam antibiotics is the
production of one or several β-lactamases (BLs), including the highly worrying …

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 …

2-Substituted 4, 5-dihydrothiazole-4-carboxylic acids are novel inhibitors of metallo-β-lactamases

P Chen, LB Horton, RL Mikulski, L Deng… - Bioorganic & medicinal …, 2012 - Elsevier
Bacterial resistance to β-lactam antibiotics caused by class B metallo-β-lactamases (MBL),
especially for certain hospital-acquired, Gram-negative pathogens, poses a significant threat …

[HTML][HTML] Structural studies of triazole inhibitors with promising inhibitor effects against antibiotic resistance metallo-β-lactamases

Z Muhammad, S Skagseth, M Boomgaren… - Bioorganic & Medicinal …, 2020 - Elsevier
Abstract Metallo-β-lactamases (MBLs) are an emerging cause of bacterial antibiotic
resistance by hydrolysing all classes of β-lactams except monobactams, and the MBLs are …

1, 2, 4‐Triazole‐3‐thione Compounds as Inhibitors of Dizinc Metallo‐β‐lactamases

L Sevaille, L Gavara, C Bebrone, F De Luca… - …, 2017 - Wiley Online Library
Abstract Metallo‐β‐lactamases (MBLs) cause resistance of Gram‐negative bacteria to β‐
lactam antibiotics and are of serious concern, because they can inactivate the last‐resort …