The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Cladinose Analogues of Sixteen-membered Macrolide Antibiotics
IV. Improved Therapeutic Effects of 4-O-Acyl-L-cladinose Analogues of Sixteen-membered Macrolide Antibiotics
KEIICHI AJITO, KEN-ICHI KURIHARA, SEIJI SHIBAHARA, OSAMU HARA, TSUNEO OKONOGI, NOBUE KIKUCHI, MINAKO ARAAKE, HISASHI SUZUKI, SHOJI OMOTO, SHIGEHARU INOUYE
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JOURNAL FREE ACCESS

1997 Volume 50 Issue 2 Pages 150-161

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Abstract

Six derivatives of sixteen-membered macrolides possessing 4-O-acyl-α-L-cladinose as a neutral sugar were synthesized via 3"-methylthiomethyl ether intermediates in reasonable yield. Introduction of a methyl group on the 3"-hydroxyl group of midecamycin A1 was effective for enhancing its antibacterial activity. All these derivatives exhibited excellent therapeutic effects in mice, and some of them showed improved pharmacokinetics compared with the natural antibiotics (mycarose type) in mice. Facile synthesis of 9-O-acylated analogues are also described.

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The Journal of Antibiotics, Series A

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