Abstract
A series of novel 11-[3-[(arylcarbamoyl)oxy]propylamino]-11-deoxy-6-O-methyl-3-oxoerythromycin A 11-N,12-O-cyclic carbamate derivatives (6a–h) were designed, synthesized and evaluated for their antibacterial activities in vitro. Most of these compounds had significant antibacterial activity against two groups of pathogens of Methicillin-sensitive Staphylococcus aureus (MIC50=0.031–2 μg ml−1) except 6g and Methicillin-sensitive S. epidermidis (MIC50=0.031–0.5 μg ml−1). MIC90 of 6d against Methicillin-resistant S. epidermidis was at least 16-fold better than that of erythromycin (EMA), azithromycin (AZM) and ABT-773. 6d and 6e had more potent antibacterial activity against S. pneumoniae than EMA, AZM and ABT-773. In particular, compounds 6d and 6e also showed relatively potent activity against Haemophilus influenzae and Streptococcus hemolyticus.
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This research was supported by Shandong Xinhua Pharmaceutical Co., Ltd., and National Natural Science Foundation of China (30801427).
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Zheng, Z., Du, D., Cao, L. et al. Synthesis and antibacterial activity of novel 11-[3-[(arylcarbamoyl)oxy]propylamino]-11-deoxy-6-O-methyl-3-oxoerythromycin A 11-N,12-O-cyclic carbamate derivatives. J Antibiot 69, 811–817 (2016). https://doi.org/10.1038/ja.2016.42
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DOI: https://doi.org/10.1038/ja.2016.42
