Cladinose Analogues of Sixteen-membered Macrolide Antibiotics. I. Synthesis of 4-0-Alkyl-L-cladinose Analogues via Glycosylation.
- 1 January 1996
- journal article
- research article
- Published by Japan Antibiotics Research Association in The Journal of Antibiotics
- Vol. 49 (6) , 582-592
- https://doi.org/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.Keywords
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