Abstract
A series of new triazole-containing ketolides and 2-fluoro-ketolides in which the 5-O-desosamine was replaced by unnatural sugars were synthesized and evaluated against relevant macrolide-sensitive and macrolide-resistant respiratory pathogens. Excellent in vitro antibacterial activities were demonstrated for ketolide analogues having the 6'-OBz-3'-dimethylamino-glucose and 6'-OBz-4'-deoxy-3'-dimethylamino-glucose substituents.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Amino Sugars / chemistry*
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Anti-Bacterial Agents* / chemical synthesis
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Anti-Bacterial Agents* / pharmacology
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Ketolides* / chemical synthesis
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Ketolides* / pharmacology
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Microbial Sensitivity Tests
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Molecular Conformation
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Amino Sugars
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Anti-Bacterial Agents
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Ketolides
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desosamine