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

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.

MeSH terms

  • Amino Sugars / chemistry*
  • Animals
  • Anti-Inflammatory Agents / chemical synthesis
  • Anti-Inflammatory Agents / therapeutic use*
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Drug Design
  • Edema / drug therapy*
  • Edema / pathology
  • Erythromycin / analogs & derivatives*
  • Erythromycin / chemical synthesis
  • Erythromycin / pharmacology
  • Erythromycin / therapeutic use*
  • Mice

Substances

  • Amino Sugars
  • Anti-Inflammatory Agents
  • desosamine
  • Erythromycin