Progress toward inhibitors of metallo-β-lactamases

RP McGeary, DTC Tan, G Schenk - Future Medicinal Chemistry, 2017 - Future Science
The global overuse of antibiotics has led to the emergence of drug-resistant pathogenic
bacteria. Bacteria can combat β-lactams by expressing β-lactamases. Inhibitors of one class …

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 …

Pharmaceutical approaches to target antibiotic resistance mechanisms

D Schillaci, V Spanò, B Parrino… - Journal of medicinal …, 2017 - ACS Publications
There is urgent need for new therapeutic strategies to fight the global threat of antibiotic
resistance. The focus of this Perspective is on chemical agents that target the most common …

Metallo-β-lactamase inhibitors by bioisosteric replacement: Preparation, activity and binding

S Skagseth, S Akhter, MH Paulsen… - European journal of …, 2017 - Elsevier
Bacterial resistance is compromising the use of β-lactam antibiotics including carbapenems.
The main resistance mechanism against β-lactams is hydrolysis of the β-lactam ring …

Challenges in the development of a thiol-based broad-spectrum inhibitor for metallo-β-lactamases

D Büttner, JS Kramer, FM Klingler… - ACS infectious …, 2017 - ACS Publications
Pathogens, expressing metallo-β-lactamases (MBLs), become resistant against most β-
lactam antibiotics. Besides the dragging search for new antibiotics, development of MBL …

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 …

Captopril/enalapril inhibit promiscuous esterase activity of carbonic anhydrase at micromolar concentrations: An in vitro study

S Esmaeili, MR Ashrafi-Kooshk, H Adibi… - Chemico-Biological …, 2017 - Elsevier
The inhibitory activity of captopril, a thiol-containing competitive inhibitor of the angiotensin-
converting enzyme, ACE, against esterase activity of carbonic anhydrase, CA was …

Structural insights into TMB-1 and the role of residues 119 and 228 in substrate and inhibitor binding

S Skagseth, T Christopeit, S Akhter… - Antimicrobial Agents …, 2017 - Am Soc Microbiol
ABSTRACT Metallo-β-lactamases (MBLs) threaten the effectiveness of β-lactam antibiotics,
including carbapenems, and are a concern for global public health. β-Lactam/β-lactamase …

Antimicrobial and Resistance-Modifying Activities of LY2183240 Regioisomers

PE De Resende - 2017 - discovery.ucl.ac.uk
The rapid development of antimicrobial resistance over the past three decades represents a
critical public health threat and urgent challenge. In this context, in order to establish lead …

An investigation of New Delhi metallo-[beta]-lactamase: clinical variants, lipid modification & inhibition

A Stewart - 2017 - repositories.lib.utexas.edu
Many β-lactam drugs, including penicillins, monobactams cephalosporins, and
carbapenems, are used in clinical treatment of bacterial infections. However, resistant …