Abstract
A series of 4''-O-acyl derivatives of 8a-aza-8a-homoerythromycins A were synthesized and tested against Gram-positive and Gram-negative bacteria. Derivatives of 8a-aza-8a-homoerythromycin A have potent anti-bacterial activity against not only azithromycin-susceptible strains, but also efflux (M) and inducible macrolide-lincosamide-streptogramin-resistant Gram-positive pathogens. These compounds show moderate to high clearance and low oral bioavailability in preliminary in vivo pharmacokinetic studies in rat.
MeSH terms
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Acylation
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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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Catalysis
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Erythromycin / analogs & derivatives*
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Erythromycin / chemical synthesis
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Erythromycin / pharmacology
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Gram-Negative Bacteria / drug effects
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Gram-Positive Bacteria / drug effects
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Indicators and Reagents
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Magnetic Resonance Spectroscopy
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Male
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Mass Spectrometry
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Rats
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Rats, Wistar
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Stereoisomerism
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Structure-Activity Relationship
Substances
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8a-aza-8a-homoerythromycin
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Anti-Bacterial Agents
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Indicators and Reagents
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Erythromycin