Abstract
From the X-ray crystal structures of linezolid and the non-selective antibiotic sparsomycin, we have derived a new family of hybrid oxazolidinones. From this initial compound set we have developed a new biaryloxazolidinone scaffold that shows both potent antimicrobial activity as well as selective inhibition of ribosomal translation. The synthesis of these compounds is outlined.
MeSH terms
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Acetamides / pharmacology
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Administration, Oral
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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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Crystallography, X-Ray
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Drug Design
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Escherichia coli / drug effects
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Haemophilus influenzae / drug effects
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Linezolid
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Microbial Sensitivity Tests
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Molecular Conformation
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Molecular Structure
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Moraxella catarrhalis / drug effects
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Oxazolidinones / chemical synthesis*
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Oxazolidinones / chemistry
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Oxazolidinones / pharmacology*
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Protein Biosynthesis / drug effects
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Sparsomycin / pharmacology
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Structure-Activity Relationship
Substances
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Acetamides
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Anti-Bacterial Agents
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Oxazolidinones
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Sparsomycin
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Linezolid