Abstract
The synthesis and antibacterial activity of (7S)-7-sulfur-azetidin-3-yl lincomycin derivatives are described. Modification was achieved by a simple reaction of (7R)-7-O-methanesulfonyllincomycin and the corresponding substituted azetidine-2-thiol. Several compounds first showed moderate antibacterial activity against Streptococcus pneumoniae and Streptococcus pyogenes with erm gene as lincomycin derivatives.
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Acknowledgements
We thank Mr A Tamura and Dr T Okutomi for valuable scientific discussion. We are grateful to Professor Emeritus Dr M Konno for supervision through our in-house drug discovery program in lincomycin field. We are also grateful to Ms T Miyara, Ms S Miki, Ms K Kaneda, Dr T Murata and Mr S Sato for contribution toward analytical chemistry, Mr T Matsuhira for biological studies, and Ms M Takagi for manuscript.
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Kumura, K., Wakiyama, Y., Ueda, K. et al. Synthesis and antibacterial activity of novel lincomycin derivatives. I. Enhancement of antibacterial activities by introduction of substituted azetidines. J Antibiot 69, 440–445 (2016). https://doi.org/10.1038/ja.2015.134
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DOI: https://doi.org/10.1038/ja.2015.134
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