Design, synthesis and in vivo activity of 9-( S)-dihydroerythromycin derivatives as potent anti-inflammatory agents

The synthesis of a new class of 9-( S)-dihydroerythromycin derivatives and their anti-inflammatory activity are reported. The synthesis of a new class of 9-( S)-dihydroerythromycin derivatives and their anti-inflammatory activity on in vivo PMA assay are described. Modifying the desosamine sugar on...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2006-11, Vol.16 (22), p.5801-5804
Hauptverfasser: Mereu, A., Moriggi, E., Napoletano, M., Regazzoni, C., Manfredini, S., Mercurio, T.P., Pellacini, F.
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Sprache:eng
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Zusammenfassung:The synthesis of a new class of 9-( S)-dihydroerythromycin derivatives and their anti-inflammatory activity are reported. The synthesis of a new class of 9-( S)-dihydroerythromycin derivatives and their anti-inflammatory activity on in vivo PMA assay are described. Modifying the desosamine sugar on the C-3′ amino group, it was possible to differentiate between anti-biotic and anti-flammatory action. The compounds are completely devoid of anti-microbial effects but their anti-inflammatory properties are enhanced. These results strongly suggest the potential of macrolides as a new class of anti-inflammatory agents.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.08.076