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

作者信息

Mereu A, Moriggi E, Napoletano M, Regazzoni C, Manfredini S, Mercurio T P, Pellacini F

机构信息

Inpharzam Ricerche S. A.; Via ai Söi, BP 328, 6807 Taverne, Switzerland.

出版信息

Bioorg Med Chem Lett. 2006 Nov 15;16(22):5801-4. doi: 10.1016/j.bmcl.2006.08.076. Epub 2006 Sep 18.

Abstract

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-inflammatory 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.

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