The intramolecular cyclizations of oxazolidinones with carbanions adjacent to sulfones, sulfoxides and phosphonates proceed in high yields to obtain functionalized γ and δ lactams. The chiral oxazolidinone precursors can be readily synthesized from commercial amino acids. The lactams from this study are useful synthetic intermediates, as demonstrated by the synthesis of a precursor for levetiracetam, an antiepileptic drug.
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http://dx.doi.org/10.1016/j.tetlet.2010.12.062 | DOI Listing |
FEMS Microbiol Lett
January 2025
Department of Bioscience and Biotechnology, Indian Institute of Technology Kharagpur, Kharagpur-721302, West Bengal, India.
Verona-integron-metallo-β-lactamase (VIM-2) is one of the most widespread class B β-lactamase responsible for β-lactam resistance. Although active-site residues help in metal binding, the residues nearing the active-site possess functional importance. Here, to decipher the role of such residues in the activity and stability of VIM-2, the residues E146, D182, N210, S207, and D213 were selected through in-silico analyses and substituted with alanine using site-directed mutagenesis.
View Article and Find Full Text PDFBMC Microbiol
January 2025
Department of Pediatrics, Institute of Medical Sciences, Banaras Hindu University, Varanasi, India.
Carbapenem resistant Acinetobacter baumannii has evolved as the most troublesome microorganism with multiple virulence factors. Biofilm formation, porins, micronutrient capturing mechanism and quorum sensing, provide protection against desiccation, host-pathogen killing and enhance its persistence. The conservation of these factors between colonizing and pathogenic carbapenem resistant A.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Group of Fungal Genetic Engineering, Federal Research Center "Fundamentals of Biotechnology" of the Russian Academy of Sciences, Leninsky Prosp. 33-2, 119071 Moscow, Russia.
From the 1950s to the present, the main tool for obtaining fungal industrial producers of secondary metabolites remains the so-called classical strain improvement (CSI) methods associated with multi-round random mutagenesis and screening for the level of target products. As a result of the application of such techniques, the yield of target secondary metabolites in high-yielding (HY) strains was increased hundreds of times compared to the wild-type (WT) parental strains. However, the events that occur at the molecular level during CSI programs are still unknown.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Department of Biology of Bacteria, Institute of Microbiology, Biotechnology and Immunology, Faculty of Biology and Environmental Protection, University of Lodz, 90-237 Lodz, Poland.
A phage-antibiotic synergy could be an alternative in urinary tract infection (UTI) therapy, as it leads to the elimination of bacteria and to the reduction in variants resistant to phages and antibiotics. The aims of the in vitro study were to determine whether phages vB_Efa29212_2e and vB_Efa29212_3e interact synergistically with selected antibiotics in the treatment of infections, to optimize antibiotic concentrations and phage titers for the most effective combinations, and to assess their impact on the number of spontaneous resistant variants and on the phages' reproductive cycles. The modified double-layer disc diffusion method, checkboard, time-kill assays, one-step growth method and the double agar overlay plaque assay were implemented.
View Article and Find Full Text PDFMolecules
December 2024
IPC-Institute for Polymers and Composites, University of Minho, 4800-056 Guimarães, Portugal.
Free pectinase is commonly employed as a biocatalyst in wine clarification; however, its removal, recovery, and reuse are not feasible. To address these limitations, this study focuses on the immobilization of a commercial pectinolytic preparation (Pec) onto highly porous polymer microparticles (MPs). Seven microparticulate polyamide (PA) supports, namely PA4, PA6, PA12 (with and without magnetic properties), and the copolymeric PA612 MP, were synthesized through activated anionic ring-opening polymerization of various lactams.
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