Abstract
A series of new 4″-O-carbamates of 11,12-cyclic carbonate erythromycin A 6,9-imino ether were synthesized and evaluated for their in vitro antibacterial activity. All the desired compounds demonstrated favorable activity (0.03 μg ml–1) against erythromycin-susceptible Streptococcus pneumoniae comparable to the references, exhibiting 133-fold higher activity than precursor 2 or 3. Similarly, all of the analogs exhibited improved activity against the erythromycin-resistant S. pneumoniae encoded by the erm gene and the erm and mef genes, showing 4–32-fold more effectiveness than erythromycin A.
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Acknowledgements
This research was supported by National Natural Science Foundation of China (21072114 and 20872081), Major R&D Program of New Drugs—National S&T Key Special Subject of China (2009ZX09103-115) and the Project-sponsored by SRF for ROCS, SEM.
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Zhang, L., Jiao, B., Yang, X. et al. Synthesis and antibacterial activity of new 4″-O-carbamates of 11,12-cyclic carbonate erythromycin A 6,9-imino ether. J Antibiot 64, 243–247 (2011). https://doi.org/10.1038/ja.2010.166
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DOI: https://doi.org/10.1038/ja.2010.166
