Synthesis and antibacterial activity of 11,12-carbamate-3-O-acyl erythromycin derivatives

Abstract

A novel series of acylide derivatives have been synthesized which exhibit in vitro potency against key respiratory pathogens. Modification of position 3 was accomplished by replacing different 3-O-substituted acyl groups in the macrolide core via a facile procedure. Compounds 7a–7i were eventually yielded by the conjunction of diverse hetero-aryl side chains with the 11-N,12-O-carbamate sub-structure.

Keywords:

• macrolide
• acylide
• antibacterial activity
• resistant strains

Acknowledgements

This work was supported by the National Natural Science Foundation of China (30572275) and Natural Science Foundation of Beijing (7062047).