Synthesis and kinetic testing of tetrahydropyrimidine‐2‐thione and pyrrole derivatives as inhibitors of the metallo‐β‐lactamase from Klebsiella pneumonia and …

WM Hussein, SS Fatahala… - Chemical biology & …, 2012 - Wiley Online Library
Metallo‐β‐lactamases (MBLs), produced by an increasing number of bacterial pathogens,
facilitate the hydrolysis of many commonly used β‐lactam antibiotics. There are no clinically …

Diversity and proliferation of metallo-β-lactamases: a clarion call for clinically effective metallo-β-lactamase inhibitors

AM Somboro, J Osei Sekyere, DG Amoako… - Applied and …, 2018 - Am Soc Microbiol
The worldwide proliferation of life-threatening metallo-β-lactamase (MBL)-producing Gram-
negative bacteria is a serious concern to public health. MBLs are compromising the …

1,4,7-Triazacyclononane Restores the Activity of β-Lactam Antibiotics against Metallo-β-Lactamase-Producing Enterobacteriaceae: Exploration of Potential Metallo-β …

AM Somboro, DG Amoako, J Osei Sekyere… - Applied and …, 2019 - Am Soc Microbiol
ABSTRACT Metallo-β-lactamase (MBL)-producing Enterobacteriaceae are of grave clinical
concern, particularly as there are no metallo-β-lactamase inhibitors approved for clinical …

Azolylthioacetamide: a highly promising scaffold for the development of metallo-β-lactamase inhibitors

SK Yang, JS Kang, P Oelschlaeger… - ACS medicinal …, 2015 - ACS Publications
A new scaffold, azolylthioacetamide, was constructed and assayed against metallo-β-
lactamases (MβLs). The obtained molecules specifically inhibited MβL ImiS, and 1c was …

Metallo-β-lactamases: structure, function, epidemiology, treatment options, and the development pipeline

SE Boyd, DM Livermore, DC Hooper… - Antimicrobial agents …, 2020 - Am Soc Microbiol
Modern medicine is threatened by the global rise of antibiotic resistance, especially among
Gram-negative bacteria. Metallo-β-lactamase (MBL) enzymes are a particular concern and …

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 …

Structure-based development of (1-(3′-mercaptopropanamido) methyl) boronic acid derived broad-spectrum, dual-action inhibitors of metallo-and serine-β …

YL Wang, S Liu, ZJ Yu, Y Lei, MY Huang… - Journal of Medicinal …, 2019 - ACS Publications
The emergence and spread of bacterial pathogens acquired metallo-β-lactamase (MBL) and
serine-β-lactamase (SBL) medicated β-lactam resistance gives rise to an urgent need for the …

2-Mercaptomethyl-thiazolidines use conserved aromatic–S interactions to achieve broad-range inhibition of metallo-β-lactamases

MA Rossi, V Martinez, P Hinchliffe, MF Mojica… - Chemical …, 2021 - pubs.rsc.org
Infections caused by multidrug resistant (MDR) bacteria are a major public health threat.
Carbapenems are among the most potent antimicrobial agents that are commercially …

Kinetic and structural characterization of the first B3 metallo-β-lactamase with an active-site glutamic acid

LA Wilson, EG Knaven, MT Morris… - Antimicrobial agents …, 2021 - Am Soc Microbiol
The structural diversity in metallo-β-lactamases (MBLs), especially in the vicinity of the active
site, has been a major hurdle in the development of clinically effective inhibitors …

Metallo-β-lactamases in the age of multidrug resistance: from structure and mechanism to evolution, dissemination, and inhibitor design

G Bahr, LJ Gonzalez, AJ Vila - Chemical reviews, 2021 - ACS Publications
Antimicrobial resistance is one of the major problems in current practical medicine. The
spread of genes coding for resistance determinants among bacteria challenges the use of …