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 …

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 …

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 …

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 …

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 …

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 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 …

Mechanistic Investigations of Metallo‐β‐lactamase Inhibitors: Strong Zinc Binding Is Not Required for Potent Enzyme Inhibition

N Wade, KHME Tehrani, NC Brüchle… - …, 2021 - Wiley Online Library
Abstract Metallo‐β‐lactamases (MBLs) are zinc‐dependent bacterial enzymes that
inactivate essentially all classes of β‐lactam antibiotics including last‐resort carbapenems …

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 …

An elusive task: a clinically useful inhibitor of metallo-β-lactamases

MM González, AJ Vila - Zinc Enzyme Inhibitors: Enzymes from …, 2017 - Springer
Multidrug-resistant bacterial infections have become in recent years an increasingly
worrisome problem in the medical community. The β-lactams are the most used antibiotics …