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

作者: KEN-ICHI KURIHARA , KEIICHI AJITO , SEIJI SHIBAHARA , TSUNEO ISHIZUKA , OSAMU HARA

DOI: 10.7164/ANTIBIOTICS.49.582

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

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