A new series of macrolide derivatives with 4''-O-saccharide substituents.

Bioorg Med Chem Lett

Key Laboratory of Bioactivity Substance and Resources Utilization of Chinese Herbal Medicine, Ministry of Education Institute of Materia Medica, Peking Union Medica College & Chinese Academy of Medical Sciences, Beijing 100050, PR China.

Published: September 2010

AI Article Synopsis

  • A new type of macrolide derivatives with 4''-O-mono- or disaccharides was created using glycosyl trichloroacetimidates for glycosylation.
  • Tests were conducted to evaluate the antibacterial effectiveness of these derivatives against both susceptible and resistant bacterial pathogens.
  • This research aims to enhance our understanding of how these modified macrolides interact with bacterial ribosomes, potentially leading to better antibacterial treatments.

Article Abstract

A series of novel derivatives of macrolide with 4''-O-mono- or disaccharides were synthesized. The corresponding glycosyl trichloroacetimidates were used as the donors in the glycosylations. The in vitro antibacterial activities of 7a-f and 13-16 against a panel of susceptible and resistant pathogens were tested. The modification of 4''-O-mono- or disaccharides may lead to the understanding of interaction of the macrolide and the bacterial ribosome.

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http://dx.doi.org/10.1016/j.bmcl.2010.07.072DOI Listing

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