Structure-based design of covalent inhibitors targeting metallo-β-lactamases.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112573
Abstract: The emergence and prevalence of metallo-β-lactamases (MβLs)-mediated bacterial resistance has seriously threatened the global health today. MβLs are deemed to be one of the most worrying bacterial resistance factors that hydrolyze nearly all β-lactam antibiotics.… read more here.
Keywords: covalent inhibitors; design covalent; covalent; metallo lactamases ... See more keywords
Stereochemically altered cephalosporins as potent inhibitors of New Delhi metallo-β-lactamases.
Sign Up to like & getrecommendations! Published in 2022 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2022.114174
Abstract: Antibiotic resistance caused by β-lactamases, particularly metallo-β-lactamases, has been a major threat to public health globally. New Delhi metallo-β-lactamase-1 (NDM-1) represents one of the most important metallo-β-lactamases; the production of NDM-1 in bacterial pathogen significantly… read more here.
Keywords: new delhi; metallo lactamases; metallo; stereochemically altered ... See more keywords
N-Aryl Mercaptopropionamides as Broad-Spectrum Inhibitors of Metallo-β-Lactamases.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01755
Abstract: Drug-resistant pathogens pose a global challenge to public health as they cause diseases that are extremely difficult to cure. Metallo-β-lactamases (MBLs) are a diverse set of zinc-containing enzymes that catalyze the hydrolysis of β-lactam drugs,… read more here.
Keywords: aryl mercaptopropionamides; inhibitors metallo; spectrum inhibitors; mercaptopropionamides broad ... See more keywords
Computational and biological profile of boronic acids for the detection of bacterial serine- and metallo-β-lactamases
Sign Up to like & getrecommendations! Published in 2017 at "Scientific Reports"
DOI: 10.1038/s41598-017-17399-7
Abstract: Abstractβ-Lactamases (BLs) able to hydrolyze β-lactam antibiotics and more importantly the last resort carbapenems, represent a major mechanism of resistance in Gram-negative bacteria showing multi-drug or extensively drug resistant phenotypes. The early detection of BLs… read more here.
Keywords: bls; detection; clinically relevant; metallo lactamases ... See more keywords
2-Mercaptomethyl-thiazolidines use conserved aromatic–S interactions to achieve broad-range inhibition of metallo-β-lactamases†
Sign Up to like & getrecommendations! Published in 2021 at "Chemical Science"
DOI: 10.1039/d0sc05172a
Abstract: Infections caused by multidrug resistant (MDR) bacteria are a major public health threat. Carbapenems are among the most potent antimicrobial agents that are commercially available to treat MDR bacteria. Bacterial production of carbapenem-hydrolysing metallo-β-lactamases (MBLs)… read more here.
Keywords: mercaptomethyl thiazolidines; thiazolidines use; use conserved; conserved aromatic ... See more keywords
Trade-Offs between Antibacterial Resistance and Fitness Cost in the Production of Metallo-β-Lactamases by Enteric Bacteria Manifest as Sporadic Emergence of Carbapenem Resistance in a Clinical Setting
Sign Up to like & getrecommendations! Published in 2021 at "Antimicrobial Agents and Chemotherapy"
DOI: 10.1128/aac.02412-20
Abstract: Meropenem is a clinically important antibacterial reserved for treatment of multiresistant infections. In meropenem-resistant bacteria of the family Enterobacterales, New Delhi metallo-β-lactamase 1 (NDM-1) is considerably more common than IMP-1, despite both metallo-β-lactamases (MBLs) hydrolyzing… read more here.
Keywords: fitness; meropenem; metallo lactamases; resistance ... See more keywords
Drug development concerning metallo-β-lactamases in gram-negative bacteria
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Microbiology"
DOI: 10.3389/fmicb.2022.959107
Abstract: β-Lactams have been a clinical focus since their emergence and indeed act as a powerful tool to combat severe bacterial infections, but their effectiveness is threatened by drug resistance in bacteria, primarily by the production… read more here.
Keywords: concerning metallo; metallo; metallo lactamases; development concerning ... See more keywords
Studies on the Reactions of Biapenem with VIM Metallo β-Lactamases and the Serine β-Lactamase KPC-2
Sign Up to like & getrecommendations! Published in 2022 at "Antibiotics"
DOI: 10.3390/antibiotics11030396
Abstract: Carbapenems are important antibacterials and are both substrates and inhibitors of some β-lactamases. We report studies on the reaction of the unusual carbapenem biapenem, with the subclass B1 metallo-β-lactamases VIM-1 and VIM-2 and the class… read more here.
Keywords: reactions biapenem; lactamase kpc; studies reactions; kpc ... See more keywords
A Modified Vancomycin Molecule Confers Potent Inhibitory Efficacy against Resistant Bacteria Mediated by Metallo-β-Lactamases
Sign Up to like & getrecommendations! Published in 2022 at "Molecules"
DOI: 10.3390/molecules27227685
Abstract: Multidrug-resistant bacterial infections mediated by metallo-β-lactamases (MβLs) have grown into an emergent health threat, and development of novel antimicrobials is an ideal strategy to combat the infections. Herein, a novel vancomycin derivative Vb was constructed… read more here.
Keywords: modified vancomycin; mediated metallo; vancomycin molecule; metallo lactamases ... See more keywords
4-Amino-1,2,4-triazole-3-thione as a Promising Scaffold for the Inhibition of Serine and Metallo-β-Lactamases
Sign Up to like & getrecommendations! Published in 2020 at "Pharmaceuticals"
DOI: 10.3390/ph13030052
Abstract: The emergence of bacteria that co-express serine- and metallo- carbapenemases is a threat to the efficacy of the available β-lactam antibiotic armamentarium. The 4-amino-1,2,4-triazole-3-thione scaffold has been selected as the starting chemical moiety in the… read more here.
Keywords: serine metallo; amino triazole; triazole thione; metallo ... See more keywords
Progress toward inhibitors of metallo-β-lactamases.
Sign Up to like & getrecommendations! Published in 2017 at "Future medicinal chemistry"
DOI: 10.4155/fmc-2017-0007
Abstract: 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 of β-lactamase, the serine-β-lactamases, are used clinically to prevent degradation… read more here.
Keywords: chemistry; toward inhibitors; progress toward; metallo lactamases ... See more keywords