Synthesis and biological investigation of new 4″-malonyl tethered derivatives of erythromycin and clarithromycin

Bioorganic & Medicinal Chemistry Letters
2006.0

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.

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