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Synthesis and biological evaluation of new N-linked 5-triazolylmethyl oxazolidinones

Authors
Journal
European Journal of Medicinal Chemistry
0223-5234
Publisher
Elsevier
Publication Date
Volume
43
Issue
8
Identifiers
DOI: 10.1016/j.ejmech.2007.09.010
Keywords
  • Oxazolidinone
  • Linezolid
  • Antibacterial Agents
  • Gram-Positive Organisms
Disciplines
  • Pharmacology

Abstract

Abstract A new series of oxazolidinones bearing N-linked 5-triazolylmethyl group have been synthesized and their in vitro antibacterial activities ( MIC) were evaluated against a spectrum of resistant and susceptible Gram-positive organisms. Some of the analogues in this series displayed activity superior to linezolid and vancomycin. Furthermore, in vivo efficacies and pharmacokinetic properties of the selected compounds were also disclosed herein; the selected compounds showed reasonable bioavailability as well as in vivo efficacy comparable to that of linezolid.

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