Ruthenium‐Catalyzed Cycloaddition for Introducing Chemical Diversity in Second‐Generation β‐Lactamase Inhibitors
Sign Up to like & getrecommendations! Published in 2023 at "ChemMedChem"
DOI: 10.1002/cmdc.202300077
Abstract: Ruthenium(II) alkyne azide cycloaddition (RuAAC) is an attractive reaction to access 1,5‐triazole derivatives and is applicable to internal alkynes. Here, we explore RuAAC to introduce molecular diversity on the diazabicyclooctane (DBO) scaffold of β‐lactamase inhibitors.… read more here.
Keywords: catalyzed cycloaddition; ruthenium catalyzed; lactamase inhibitors; diversity ... See more keywords
Probing transport of charged β-lactamase inhibitors through OmpC, a membrane channel from E. coli.
Sign Up to like & getrecommendations! Published in 2017 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2017.01.076
Abstract: One of the major causes of antibiotic resistance in the Gram-negative bacteria is the low permeability across the outer membrane. Currently a main bottleneck in the development of effective antibiotics is the lack of a… read more here.
Keywords: lactamase inhibitors; transport charged; inhibitors ompc; probing transport ... See more keywords
Rapid Evolution of a Fragment-like Molecule to Pan-Metallo-Beta-Lactamase Inhibitors: Initial Leads toward Clinical Candidates.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00766
Abstract: With the emergence and rapid spreading of NDM-1 and existence of clinically relevant VIM-1 and IMP-1, discovery of pan inhibitors targeting metallo-beta-lactamases (MBLs) became critical in our battle against bacterial infection. Concurrent with our fragment… read more here.
Keywords: beta; chemistry; beta lactamase; lactamase inhibitors ... See more keywords
In Silico Fragment-Based Design Identifies Subfamily B1 Metallo-β-lactamase Inhibitors.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b01728
Abstract: Zinc ion-dependent β-lactamases (MBLs) catalyze the hydrolysis of almost all β-lactam antibiotics and resist the action of clinically available β-lactamase inhibitors. We report how application of in silico fragment-based molecular design employing thiol-mediated metal anchorage… read more here.
Keywords: lactamase inhibitors; mbl; fragment based; silico fragment ... See more keywords
Traceless Staudinger Ligation To Introduce Chemical Diversity on β-Lactamase Inhibitors of Second Generation.
Sign Up to like & getrecommendations! Published in 2021 at "Organic letters"
DOI: 10.1021/acs.orglett.1c02741
Abstract: We explored the traceless Staudinger ligation for the functionalization of the C2 position of second generation β-lactamase inhibitors based on a diazabicyclooctane (DBO) scaffold. Our strategy is based on the synthesis of phosphine phenol esters… read more here.
Keywords: staudinger ligation; traceless staudinger; second generation; lactamase inhibitors ... See more keywords
SAR Studies Leading to the Identification of a Novel Series of Metallo-β-lactamase Inhibitors for the Treatment of Carbapenem-Resistant Enterobacteriaceae Infections That Display Efficacy in an Animal Infection Model
Sign Up to like & getrecommendations! Published in 2019 at "ACS Infectious Diseases"
DOI: 10.1021/acsinfecdis.8b00246
Abstract: The clinical effectiveness of carbapenem antibiotics such as meropenem is becoming increasingly compromised by the spread of both metallo-β-lactamase (MBL) and serine-β-lactamase (SBL) enzymes on mobile genetic elements, stimulating research to find new β-lactamase inhibitors… read more here.
Keywords: carbapenem; metallo lactamase; series metallo; lactamase inhibitors ... See more keywords
β-lactam/β-lactamase inhibitor combinations: an update.
Sign Up to like & getrecommendations! Published in 2018 at "MedChemComm"
DOI: 10.1039/c8md00342d
Abstract: Antibiotic resistance caused by β-lactamase production continues to present a growing challenge to the efficacy of β-lactams and their role as the most important class of clinically used antibiotics. In response to this threat however,… read more here.
Keywords: lactamase inhibitors; class; inhibitor combinations; lactam lactamase ... See more keywords
Catalytic asymmetric total synthesis of diazabicyclooctane β-lactamase inhibitors avibactam and relebactam.
Sign Up to like & getrecommendations! Published in 2022 at "Chemical communications"
DOI: 10.1039/d2cc04006a
Abstract: A catalytic asymmetric total synthesis of avibactam and relebactam, two marketed diazabicyclooctane (DBO) β-lactamase inhibitors (BLIs), has been accomplished. An important feature of this study is the creation of a stereogenic center by using Rh-catalysed… read more here.
Keywords: avibactam relebactam; lactamase inhibitors; asymmetric total; total synthesis ... See more keywords
Penicillin-Binding Protein Occupancy Dataset for 18 β-Lactams and 4 β-Lactamase Inhibitors in Neisseria gonorrhoeae
Sign Up to like & getrecommendations! Published in 2023 at "Microbiology Spectrum"
DOI: 10.1128/spectrum.00692-23
Abstract: The manuscript represents the first N. gonorrhoeae PBP-binding data set for 22 chemically different drugs in two type strains with different genetic background. We have identified three clusters of drugs according to their PBP binding… read more here.
Keywords: binding data; lactamase inhibitors; pbp; pbp binding ... See more keywords
Discovery of Quercetin and Its Analogs as Potent OXA-48 Beta-Lactamase Inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2022.926104
Abstract: Carbapenem resistance in Enterobacteriaceae caused by OXA-48 β-lactamase is a growing global health threat and has rapidly spread in many regions of the world. Developing inhibitors is a promising way to overcome antibiotic resistance. However,… read more here.
Keywords: potent; oxa; lactamase inhibitors; discovery quercetin ... See more keywords
Use of Novel Antibiograms to Determine the Need for Earlier Susceptibility Testing and Administration for New β-Lactam/β-Lactamase Inhibitors in the United States
Sign Up to like & getrecommendations! Published in 2022 at "Antibiotics"
DOI: 10.3390/antibiotics11050660
Abstract: Antimicrobial resistance is a global public health threat, and gram-negative bacteria, such as Enterobacterales and Pseudomonas aeruginosa, are particularly problematic with difficult-to-treat resistance phenotypes. To reduce morbidity and mortality, a reduction in the time to… read more here.
Keywords: lactam lactamase; susceptibility testing; susceptibility; lactamase inhibitors ... See more keywords