The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Cladinose Analogues of Sixteen-membered Macrolide Antibiotics
I. Synthesis of 4-O-Alkyl-L-cladinose Analogues via Glycosylation
KEN-ICHI KURIHARAKEIICHI AJITOSEIJI SHIBAHARATSUNEO ISHIZUKAOSAMU HARAMINAKO ARAAKESHOJI OMOTO
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1996 Volume 49 Issue 6 Pages 582-592

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Abstract

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 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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© Japan Antibiotics Research Association
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