Abstract
We have developed a first generation of hybrid sparsomycin-linezolid compounds into a new family of orally bioavailable biaryloxazolidinones that have activity against both linezolid-susceptible and -resistant gram-positive bacteria as well as the fastidious gram-negative bacteria Haemophilus influenzae and Moraxella catarrahalis. The convergent synthesis of these new compounds is detailed.
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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Gram-Negative Bacteria / drug effects
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Gram-Positive Bacteria / 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 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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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