The Rise of Boron-Containing Compounds: Advancements in Synthesis, Medicinal Chemistry, and Emerging Pharmacology

RJ Grams, WL Santos, IR Scorei, A Abad-García… - Chemical …, 2024 - ACS Publications
Boron-containing compounds (BCC) have emerged as important pharmacophores. To date,
five BCC drugs (including boronic acids and boroles) have been approved by the FDA for …

Metallo-β-lactamase-mediated antimicrobial resistance and progress in inhibitor discovery

Y Yang, YH Yan, CJ Schofield, A McNally, Z Zong… - Trends in …, 2023 - cell.com
Resistance to β-lactam antibiotics is rapidly growing, substantially due to the spread of
serine-β-lactamases (SBLs) and metallo-β-lactamases (MBLs), which efficiently catalyse β …

β-Lactamase inhibitors to restore the efficacy of antibiotics against superbugs

C Gonzalez-Bello, D Rodríguez, M Pernas… - Journal of medicinal …, 2019 - ACS Publications
Infections caused by resistant bacteria are nowadays too common, and some pathogens
have even become resistant to multiple types of antibiotics, in which case few or even no …

New carbapenemase inhibitors: clearing the way for the β-lactams

JC Vázquez-Ucha, J Arca-Suárez, G Bou… - International journal of …, 2020 - mdpi.com
Carbapenem resistance is a major global health problem that seriously compromises the
treatment of infections caused by nosocomial pathogens. Resistance to carbapenems …

β-lactam antibiotics and β-lactamase enzymes inhibitors, part 2: our limited resources

S Alfei, AM Schito - Pharmaceuticals, 2022 - mdpi.com
β-lactam antibiotics (BLAs) are crucial molecules among antibacterial drugs, but the
increasing emergence of resistance to them, developed by bacteria producing β-lactamase …

[HTML][HTML] Protein electrostatics: From computational and structural analysis to discovery of functional fingerprints and biotechnological design

F Vascon, M Gasparotto, M Giacomello… - Computational and …, 2020 - Elsevier
Computationally driven engineering of proteins aims to allow them to withstand an extended
range of conditions and to mediate modified or novel functions. Therefore, it is crucial to the …

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 …

Recent advances in β-lactamase inhibitor chemotypes and inhibition modes

R Li, X Chen, C Zhou, QQ Dai, L Yang - European journal of medicinal …, 2022 - Elsevier
The effectiveness of β-lactam antibiotics is increasingly influenced by serine β-lactamases
(SBLs) and metallo-β-lactamases (MBLs), which can hydrolyze β-lactam antibiotics. The …

Principles and current strategies targeting metallo‐β‐lactamase mediated antibacterial resistance

YH Yan, G Li, GB Li - Medicinal Research Reviews, 2020 - Wiley Online Library
Resistance to β‐lactam antibacterials is commonly associated with the production of the
serine β‐lactamases (SBLs) and/or metallo‐β‐lactamases (MBLs). Although clinically useful …

Structure and mechanism-guided design of dual serine/metallo-carbapenemase inhibitors

C Chen, P Oelschlaeger, D Wang, H Xu… - Journal of Medicinal …, 2022 - ACS Publications
Serine/metallo-carbapenemase-coproducing pathogens, often referred to as “superbugs”,
are a significant clinical problem. They hydrolyze nearly all available β-lactam antibiotics …