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 …

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 …

[PDF][PDF] Advanced research for physico-chemical properties and parameters of toxicity piperazinium 2-((5-(furan-2-YL)-4-phenyl-4H-1, 2, 4-triazol-3-YL) THIO) acetate

Y Karpenko, Y Hunchak, B Gutyj… - ScienceRise …, 2022 - papers.ssrn.com
ADVANCED RESEARCH FOR PHYSICO-CHEMICAL PROPERTIES AND PARAMETERS OF
TOXICITY PIPERAZINIUM 2-((5-(FURAN-2-YL)-4-PHENYL-4H-1,2,4-T Page 1 ScienceRise …

Multidrug Resistant Acinetobacter baumannii Biofilms: Evaluation of Phenotypic–Genotypic Association and Susceptibility to Cinnamic and Gallic Acids

MM Sherif, WF Elkhatib, WS Khalaf… - Frontiers in …, 2021 - frontiersin.org
Acinetobacter baumannii armed with multidrug resistance (MDR) and biofilm-forming ability
is increasingly recognized as an alarming pathogen. A deeper comprehension of the …

Virtual screening identifies broad-spectrum β-lactamase inhibitors with activity on clinically relevant serine- and metallo-carbapenemases

F Spyrakis, M Santucci, L Maso, S Cross… - Scientific Reports, 2020 - nature.com
Bacteria are known to evade β-lactam antibiotic action by producing β-lactamases (BLs),
including carbapenemases, which are able to hydrolyze nearly all available β-lactams. The …

[HTML][HTML] Approachable Synthetic Methodologies for Second-Generation β-Lactamase Inhibitors: A Review

N Fatima, S Khalid, N Rasool, M Imran, B Parveen… - Pharmaceuticals, 2024 - mdpi.com
Some antibiotics that are frequently employed are β-lactams. In light of the hydrolytic
process of β-lactamase, found in Gram-negative bacteria, inhibitors of β-lactamase (BLIs) …

[HTML][HTML] Synthesis and evaluation of 1, 2, 3-triazole benzoate derivatives for inhibition of serine β-lactamases in extensively drug resistant pathogenic E. coli strains

HS Oman, AA Kharat, PS Phatak, KP Haval… - European Journal of …, 2023 - Elsevier
The β-lactamase enzyme is a leading cause of drug resistance developed by bacteria. The
combination of β-lactam (BL) antibiotics with an appropriate β-lactamase inhibitor (BLI) is a …

4-(N-Alkyl- and -Acyl-amino)-1,2,4-triazole-3-thione Analogs as Metallo-β-Lactamase Inhibitors: Impact of 4-Linker on Potency and Spectrum of Inhibition

L Gavara, F Verdirosa, A Legru, PS Mercuri, L Nauton… - Biomolecules, 2020 - mdpi.com
To fight the increasingly worrying bacterial resistance to antibiotics, the discovery and
development of new therapeutics is urgently needed. Here, we report on a new series of 1 …

N-[1,3-Dialkyl(aryl)-2-oxoimidazolidin-4-ylidene]-aryl(alkyl)sulphonamides as Novel Selective Human Cannabinoid Type 2 Receptor (hCB2R) Ligands; Insights into …

E Gianquinto, F Sodano, B Rolando, M Kostrzewa… - Molecules, 2022 - mdpi.com
Cannabinoid type 1 (hCB1) and type 2 (hCB2) receptors are pleiotropic and crucial targets
whose signaling contributes to physiological homeostasis and its restoration after injury …

Can we exploit β-lactamases intrinsic dynamics for designing more effective inhibitors?

E Gianquinto, D Tondi, G D'Arrigo, L Lazzarato… - Antibiotics, 2020 - mdpi.com
β-lactamases (BLs) represent the most frequent cause of antimicrobial resistance in Gram-
negative bacteria. Despite the continuous efforts in the development of BL inhibitors (BLIs) …