Cladinose analogues of sixteen-membered macrolide antibiotics. I. Synthesis of 4-O-alkyl-L-cladinose analogues via glycosylation

  • J Antibiot (Tokyo). 1996 Jun;49(6):582-92. doi: 10.7164/antibiotics.49.582.
K Kurihara  1 ,  K Ajito ,  S Shibahara ,  T Ishizuka ,  O Hara ,  M Araake ,  S Omoto
Affiliations
  • 1. Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., Yokohama, Japan.
PMID: 8698643 DOI: 10.7164/antibiotics.49.582
Abstract

The synthesis and biological evaluation of sixteen-membered macrolides possessing a 4-O-alkyl-alpha-L-cladinosyl moiety as the neutral sugar are described. The nine novel derivatives have been synthesized by glycosylation with 1-thio sugars. The most active derivative of them showed prolonged Antibacterial activity in rat plasma in vitro and improved pharmacokinetics.

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