Abstract
A new approach to 4''-substituted derivatives of erythromycin and clarithromycin was developed by converting them into corresponding 4''-malonic monoesters. Subsequent carbodiimide coupling with alcohols and amines provided new macrolide derivatives that are capable of binding to 50S ribosomal subunits and inhibiting protein synthesis in cell-free system.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Cell-Free System
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Clarithromycin / analogs & derivatives
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Clarithromycin / chemical synthesis*
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Clarithromycin / metabolism
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Erythromycin / analogs & derivatives
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Erythromycin / chemical synthesis*
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Erythromycin / metabolism
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Protein Synthesis Inhibitors / chemical synthesis
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Protein Synthesis Inhibitors / metabolism
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RNA, Ribosomal, 23S / metabolism
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Ribosomes / drug effects
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Ribosomes / metabolism*
Substances
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Protein Synthesis Inhibitors
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RNA, Ribosomal, 23S
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Erythromycin
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Clarithromycin