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

Article abstract of DOI:10.7164/antibiotics.49.582

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