Abstract
Substitution of phenyl oxazolidinones with carbon-linked azoles resulted in the discovery of a new class of potent oxazolidinones that have excellent Gram-positive activity. In addition, replacement of the C-5 acetamide side chains with a 4-methyl triazole diminished monoamine oxidase activity. The synthesis and biological evaluation of these compounds are reported.
MeSH terms
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Animals
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Anti-Bacterial Agents / chemical synthesis*
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Anti-Bacterial Agents / pharmacokinetics
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Anti-Bacterial Agents / pharmacology*
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Biological Availability
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Colony Count, Microbial
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Female
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Gram-Positive Bacteria / drug effects
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Half-Life
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Humans
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Liver / enzymology
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Mice
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Mice, Inbred C57BL
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Microbial Sensitivity Tests
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Monoamine Oxidase Inhibitors / chemical synthesis
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Monoamine Oxidase Inhibitors / pharmacology
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Oxazolidinones / chemical synthesis*
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Oxazolidinones / pharmacology*
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Pneumococcal Infections / drug therapy
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Pneumococcal Infections / microbiology
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Rats
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Streptococcus pneumoniae / drug effects
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Structure-Activity Relationship
Substances
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Anti-Bacterial Agents
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Monoamine Oxidase Inhibitors
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Oxazolidinones