4‴-N-demethylspiramycin derivatives: Synthesis and evaluation of effectiveness against drug-resistant bacteria

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Abstract

18-Amino-4″-O-benzoyl-4‴-N-demethyl-18-deoxospiramycins were designed and synthesized. Synthetic strategy involved selective demethylation of the dimethylamino group in forosamine, benzoylation of the hydroxyl group at the C4″ position and reductive N-amination of the formyl group. Antibacterial characteristics of spiramycin derivatives were tested. The derivatives exhibited promising activity against drug-resistant bacterial strains. © Japan Antibiotics Research Association.

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Sunazuka, T., Shudo, H., Nagai, K., Yoshida, K., Yamaguchi, Y., Hanaki, H., & Omura, S. (2008). 4‴-N-demethylspiramycin derivatives: Synthesis and evaluation of effectiveness against drug-resistant bacteria. Journal of Antibiotics, 61(3), 175–184. https://doi.org/10.1038/ja.2008.127

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