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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anti-Bacterial Agents / chemical synthesis*
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology*
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Aza Compounds / chemical synthesis*
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Aza Compounds / chemistry
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Aza Compounds / pharmacology*
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Gram-Positive Bacteria / drug effects
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Gram-Positive Bacteria / isolation & purification
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Methylation
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Mice
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Molecular Structure
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Oxazolidinones / chemical synthesis*
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Oxazolidinones / chemistry
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Oxazolidinones / pharmacology*
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Structure-Activity Relationship
Substances
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Anti-Bacterial Agents
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Aza Compounds
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Oxazolidinones