Dipicolinic acid derivatives as inhibitors of New Delhi metallo-β-lactamase-1

AY Chen, PW Thomas, AC Stewart… - Journal of medicinal …, 2017 - ACS Publications
The efficacy of β-lactam antibiotics is threatened by the emergence and global spread of
metallo-β-lactamase (MBL) mediated resistance, specifically New Delhi metallo-β-lactamase …

((S)-3-Mercapto-2-methylpropanamido) acetic acid derivatives as metallo-β-lactamase inhibitors: synthesis, kinetic and crystallographic studies

S Liu, L Jing, ZJ Yu, C Wu, Y Zheng, E Zhang… - European Journal of …, 2018 - Elsevier
The emergence and global spread of metallo-β-lactamase (MBL) mediated resistance to
almost all β-lactam antibacterials poses a serious threat to public health. Since no clinically …

Approved drugs containing thiols as inhibitors of metallo-β-lactamases: strategy to combat multidrug-resistant bacteria

FM Klingler, TA Wichelhaus, D Frank… - Journal of medicinal …, 2015 - ACS Publications
Resistance to β-lactam antibiotics can be mediated by metallo-β-lactamase enzymes
(MBLs). An MBL inhibitor could restore the effectiveness of β-lactams. We report on the …

Discovery of a novel covalent non-β-lactam inhibitor of the metallo-β-lactamase NDM-1

T Christopeit, A Albert, HKS Leiros - Bioorganic & medicinal chemistry, 2016 - Elsevier
The inhibition of metallo-β-lactamases (MBL) can prevent the hydrolysis of β-lactam
antibiotics and hence is a promising strategy for the treatment of antibiotic resistant …

Structure-activity relationship study and optimisation of 2-aminopyrrole-1-benzyl-4, 5-diphenyl-1H-pyrrole-3-carbonitrile as a broad spectrum metallo-β-lactamase …

RP McGeary, DTC Tan, C Selleck, MM Pedroso… - European Journal of …, 2017 - Elsevier
A SAR study on derivatives of 2-amino-1-benzyl-4, 5-diphenyl-1 H-pyrrole-3-carbonitrile 5a
revealed that the 3-carbonitrile group, vicinal 4, 5-diphenyl and N-benzyl side chains of the …

Design, synthesis, and in vitro and biological evaluation of potent amino acid-derived thiol inhibitors of the metallo-β-lactamase IMP-1

OK Arjomandi, WM Hussein, P Vella, Y Yusof… - European Journal of …, 2016 - Elsevier
There are currently no clinically available inhibitors of metallo-β-lactamases (MBLs). These
enzymes confer resistance to bacteria against a broad range of commonly used β-lactam …

Structure-based virtual screening for the discovery of novel inhibitors of New Delhi metallo-β-lactamase-1

F Spyrakis, G Celenza, F Marcoccia… - ACS medicinal …, 2018 - ACS Publications
Bacterial resistance has become a worldwide concern after the emergence of metallo-β-
lactamases (MBLs). They represent one of the major mechanisms of bacterial resistance …

Optimization of novel monobactams with activity against carbapenem-resistant Enterobacteriaceae–identification of LYS228

F Reck, A Bermingham, J Blais, V Capka… - Bioorganic & medicinal …, 2018 - Elsevier
Abstract Metallo-β-lactamases (MBLs), such as New Delhi metallo-β-lactamase (NDM-1)
have spread world-wide and present a serious threat. Expression of MBLs confers …

Synthesis and preclinical evaluation of TPA-based zinc chelators as metallo-β-lactamase inhibitors

C Schnaars, G Kildahl-Andersen… - ACS Infectious …, 2018 - ACS Publications
The rise of antimicrobial resistance (AMR) worldwide and the increasing spread of multi-
drug-resistant organisms expressing metallo-β-lactamases (MBL) require the development …

Synthesis and kinetic testing of new inhibitors for a metallo-β-lactamase from Klebsiella pneumonia and Pseudomonas aeruginosa

MS Mohamed, WM Hussein, RP McGeary… - European journal of …, 2011 - Elsevier
There are currently no clinically useful inhibitors against metallo-β-lactamases (MBLs),
enzymes that confer resistance against a broad spectrum of commonly used antibiotics and …