Abstract
A set of 17 novel ketolides bearing an aryltetrazolyl-substituted alkyl side chain were synthesized and evaluated for their antibacterial activities, which the aryltetrazolyl group was selected to replace the hetero-aryl moiety of the side chain in telithromycin for designing new compounds. The synthesis of aryltetrazolyl alkylamines was reported in detail. The antibacterial activities of new ketolides were evaluated against a number of pathogens including macrolide-resistant organisms by using telithromycin as the reference. Many of the evaluated compounds exhibited remarkable activities against both erythromycin-susceptible and erythromycin-resistant organisms such as Staphylococcus aureus (except S. aureus AD-08), Pseudomonas aeruginosa and Escherichia coli. Among these, the compound 11e exhibited excellent antibacterial potency against all the strains in comparison with others.
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Acknowledgements
This research work was supported in part by grants from the Natural Science Foundation of Guangdong Province (No. 06025150) and the Fundamental Research Funds for the Central Universities (No. 21610405), China. We would like to thank Professor Qi-Dong You of China Pharmaceutical University for offering the sample of telithromycin.
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Song, QL., Guo, BQ., Zhang, W. et al. Design, synthesis and antibacterial activity of novel ketolides bearing an aryltetrazolyl-substituted alkyl side chain. J Antibiot 64, 571–581 (2011). https://doi.org/10.1038/ja.2011.50
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DOI: https://doi.org/10.1038/ja.2011.50
