Abstract
Reductive aminations of the aldehyde group at C-20 position of tylosin and demycarosyltylosin (desmycosin) were carried out using primary and secondary amines in the presence of sodium cyanoborohydride. Some of these derivatives brought about higher antimicrobial and ribosome-binding activities, and the structure-activity relationship is discussed.
MeSH terms
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Animals
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Anti-Bacterial Agents / chemical synthesis*
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Indicators and Reagents
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Leucomycins / chemical synthesis*
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Leucomycins / toxicity
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Magnetic Resonance Spectroscopy
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Mass Spectrometry
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Mice
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Microbial Sensitivity Tests
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Ribosomes / drug effects
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Ribosomes / metabolism
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Structure-Activity Relationship
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Tylosin
Substances
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Anti-Bacterial Agents
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Indicators and Reagents
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Leucomycins
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4'-dexydemycarosyltylosin
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Tylosin