2 Oxazolidinones
Mostrando 1-12 de 16 artigos, teses e dissertações.
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1. Synthesis of 2-oxazolidinones with potential antibacterial activity from Morita-Baylis-Hillman adducts / Sintese de 2-oxazolidinonas com potencial atividade antibacteriana, a partir de adutos de Morita-Baylis-Hillman
Este trabalho teve como objetivo sintetizar e avaliar a atividade biológica de algumas 2-oxazolidinonas. As oxazolidinonas são compostos versáteis utilizados na preparação de uma série de outras classes de compostos e são largamente utilizados como auxiliares quirais em sínteses orgânicas assimétricas. Biologicamente são de grande importância por
Publicado em: 2007
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2. Multicenter assessment of the linezolid spectrum and activity using the disk diffusion and Etest methods: report of the Zyvox® Antimicrobial Potency Study in Latin America (LA-ZAPS)
Linezolid was the first clinically applied member of the new antimicrobial class called the "oxazolidinones". These agents have a powerful spectrum of activity focussed against Gram-positive organisms including strains with documented resistances to other antimicrobial classes. We conducted a multicenter surveillance (Zyvox Antimicrobial Potency Study; ZAPS)
Brazilian Journal of Infectious Diseases. Publicado em: 2002-06
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3. Adição diastereosseletiva de nucleofilos de carbono a ions N-aciliminios ciclicos: Aplicação na síntese de sistemas pirrolizidínico e indolizidínico monosubstituidos
Good diastereoeselection was observed in the addition of the carbon nucleophiles derived from S-tert-butyl thiopropionate 84, S-phenyl thiopropionate 96 and tert-butyl propionate 95 to the 6-membered N-acyliminium ion derived from 2-ethoxy carbamate 80. The 2RS, 1 SR relative stereochemistry of the major isomer formed in the addition of O-silylketeneacetal d
Publicado em: 1998
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4. Activities of the Oxazolidinones Linezolid and Eperezolid in Experimental Intra-Abdominal Abscess Due to Enterococcus faecalis or Vancomycin-Resistant Enterococcus faecium
The in vivo effectiveness of oxazolidinones eperezolid (U-100592) and linezolid (U-100766) against one strain each of Enterococcus faecalis and vancomycin-resistant Enterococcus faecium was examined in a rat model of intra-abdominal abscess. MICs of both drugs were 2 μg/ml for each strain. At doses of 25 mg/kg of body weight twice daily intravenously or ora
American Society for Microbiology.
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5. In vitro antimicrobial activities and spectra of U-100592 and U-100766, two novel fluorinated oxazolidinones.
Two new fluorinated oxazolidinones, U-100592 and U-100766, were evaluated against more than 659 gram-positive and -negative organisms and compared with glycopeptides, erythromycin, clindamycin, clinafloxacin, and chloramphenicol. U-100592 and U-100766 were usually equally potent, but the MICs at which 90% of the isolates are inhibited (MIC90s) of U-100592 fo
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6. Mechanism of action of oxazolidinones: effects of linezolid and eperezolid on translation reactions.
The oxazolidinones are a new class of synthetic antibiotics with good activity against gram-positive pathogenic bacteria. Experiments with a susceptible Escherichia coli strain, UC6782, demonstrated that in vivo protein synthesis was inhibited by both eperezolid (formerly U-100592) and linezolid (formerly U-100766). Both linezolid and eperezolid were potent
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7. In vitro activities of oxazolidinones U-100592 and U-100766 against penicillin-resistant and cephalosporin-resistant strains of Streptococcus pneumoniae.
Two oxazolidinones and ceftriaxone, imipenem, rifampin, and vancomycin were tested against 162 penicillin-intermediate and 68 penicillin-resistant strains of pneumococci. U-100592 is two- to fourfold more active than U-100766 against penicillin-resistant pneumococci. The MICs of U-100592 at which 90% of the isolates were inhibited were 0.25 and 0.5 microgram
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8. The Oxazolidinone Linezolid Inhibits Initiation of Protein Synthesis in Bacteria
The oxazolidinones represent a new class of antimicrobial agents which are active against multidrug-resistant staphylococci, streptococci, and enterococci. Previous studies have demonstrated that oxazolidinones inhibit bacterial translation in vitro at a step preceding elongation but after the charging of N-formylmethionine to the initiator tRNA molecule. Th
American Society for Microbiology.
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9. Activities of RPR 106972 (a new oral streptogramin), cefditoren (a new oral cephalosporin), two new oxazolidinones (U-100592 and U-100766), and other oral and parenteral agents against 203 penicillin-susceptible and -resistant pneumococci.
Agar dilution was used to determine the MICs of RPR 106972 (a new oral streptogramin), cefditoren (a new oral cephalosporin), two new oxazolidinones (U-100592 and U-100766), and other oral and parenteral agents for 203 penicillin-susceptible and -resistant pneumococci. All pneumococci were inhibited by RPR 106972 at < or = 0.5 microgram/ml. Cefditoren was ve
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10. In vitro activities of U-100592 and U-100766, novel oxazolidinone antibacterial agents.
Oxazolidinones make up a relatively new class of antimicrobial agents which possess a unique mechanism of bacterial protein synthesis inhibition. U-100592 (S)-N-[[3-[3-fluoro-4-[4-(hydroxyacetyl)-1-piperazinyl]- phenyl]-2-oxo-5-oxazolidinyl]methyl]-acetamide and U-100766 (S)-N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]- 2-oxo-5-oxazolidinyl]methyl]-acetamide are
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11. Oxazolidinones, a new class of synthetic antibacterial agents: in vitro and in vivo activities of DuP 105 and DuP 721.
DuP 721 (p-acetylphenyloxooxazolidinylmethylacetamide) and DuP 105 (a methylsulfinyl derivative) are orally active representatives of the oxazolidinones, a new class of synthetic antibacterial agents. Their antibacterial spectrum includes staphylococci, streptococci, and Bacteroides fragilis strains. The compounds have equal activity against staphylococcal s
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12. Novel Ribosomal Mutations in Staphylococcus aureus Strains Identified through Selection with the Oxazolidinones Linezolid and Torezolid (TR-700)▿
TR-700 (torezolid), the active moiety of the novel oxazolidinone phosphate prodrug TR-701, is highly potent against gram-positive pathogens, including strains resistant to linezolid (LZD). Here we investigated the potential of Staphylococcus aureus strains ATCC 29213 (methicillin-susceptible S. aureus [MSSA]) and ATCC 33591 (methicillin-resistant S. aureus [
American Society for Microbiology (ASM).