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 …

β-Lactam antibiotic targets and resistance mechanisms: from covalent inhibitors to substrates

M Mora-Ochomogo, CT Lohans - RSC Medicinal Chemistry, 2021 - pubs.rsc.org
The β-lactams are the most widely used antibacterial agents worldwide. These antibiotics, a
group that includes the penicillins and cephalosporins, are covalent inhibitors that target …

Structural characterization of the D179N and D179Y variants of KPC-2 β-lactamase: Ω-loop destabilization as a mechanism of resistance to ceftazidime-avibactam

TA Alsenani, SL Viviani, V Kumar… - Antimicrobial Agents …, 2022 - Am Soc Microbiol
Klebsiella pneumoniae carbapenemases (KPC-2 and KPC-3) present a global clinical
threat, as these β-lactamases confer resistance to carbapenems and oxyimino …

QPX7728, an ultra-broad-spectrum B-lactamase inhibitor for intravenous and oral therapy: overview of biochemical and microbiological characteristics

O Lomovskaya, R Tsivkovski, D Sun, R Reddy… - Frontiers in …, 2021 - frontiersin.org
QPX7728 is a novel β-lactamase inhibitor (BLI) that belongs to a class of cyclic boronates.
The first member of this class, vaborbactam, is a BLI in the recently approved Vabomere …

Characteristics of antibiotic resistance mechanisms and genes of Klebsiella pneumoniae

Y Li, S Kumar, L Zhang, H Wu, H Wu - Open Medicine, 2023 - degruyter.com
Klebsiella pneumoniae is an important multidrug-resistant (MDR) pathogen that can cause a
range of infections in hospitalized patients. With the growing use of antibiotics, MDR K …

2-Mercaptomethyl thiazolidines (MMTZS) inhibit all metallo-β-lactamase classes by maintaining a conserved binding mode

P Hinchliffe, DM Moreno, MA Rossi… - ACS infectious …, 2021 - ACS Publications
Metallo-β-lactamase (MBL) production in Gram-negative bacteria is an important contributor
to β-lactam antibiotic resistance. Combining β-lactams with β-lactamase inhibitors (BLIs) is a …

Recent developments to cope the antibacterial resistance via β-lactamase inhibition

Z Iqbal, J Sun, H Yang, J Ji, L He, L Zhai, J Ji, P Zhou… - Molecules, 2022 - mdpi.com
Antibacterial resistance towards the β-lactam (BL) drugs is now ubiquitous, and there is a
major global health concern associated with the emergence of new β-lactamases (BLAs) as …

Bicyclic boronate β‐lactamase inhibitors: the present hope against deadly bacterial pathogens

E Lence, C González‐Bello - Advanced Therapeutics, 2021 - Wiley Online Library
The use of β‐lactamase inhibitors in combination with β‐lactam antibiotics is an emerging
area in drug discovery. This strategy allows the restoration of the therapeutic efficacy of …

Overcoming Klebsiella pneumoniae antibiotic resistance: new insights into mechanisms and drug discovery

TXN Huy - Beni-Suef University Journal of Basic and Applied …, 2024 - Springer
Background Due to antibiotic overuse, numerous organisms have evolved multidrug
resistance, a global health crisis. Klebsiella pneumoniae (K. pneumoniae) causes …

Bicyclic Boronates as Potent Inhibitors of AmpC, the Class C β-Lactamase from Escherichia coli

PA Lang, A Parkova, TM Leissing, K Calvopiña, R Cain… - Biomolecules, 2020 - mdpi.com
Resistance to β-lactam antibacterials, importantly via production of β-lactamases, threatens
their widespread use. Bicyclic boronates show promise as clinically useful, dual-action …