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A series of novel acylide derivatives have been synthesized from clarithromycin A via a facile procedure. The C-3 modifications involved replacing the natural C-3 cladinosyl group in clarithromycin core with different aryl-piperzine sidechain via chemical synthesis.Meanwhile a distinctive intermediate with 10,11-epoxy moiety was obtained.The structure and stereochemistry of this novel structure were confirmed via NMR and X-ray crystallography.Potential anti-bacterial activities against both Grampositive and Gram-negative bacteria were reported.Because of existence of C10,11-epoxide,these derivatives can be used as intermediates for further structural modification.
A series of novel acylide derivatives have been synthesized from clarithromycin A via a facile procedure. The C-3 modifications involve replacing the natural C-3 cladinosyl group in clarithromycin core with different aryl-piperzine sidechain via chemical synthesis. Briefly, a distinctive intermediate with 10 , 11-Epoxy moiety was obtained. The structure and stereochemistry of this novel structure were confirmed by NMR and X-ray crystallography. Potential anti-bacterial activities against both Gram-negative bacteria were reported. epoxide, these derivatives can be used as intermediates for further structural modification.