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 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.
Mereu
A
A
Inpharzam Ricerche S. A.; Via ai Söi, BP 328, 6807 Taverne, Switzerland. andrea.mereu@zambongroup.com
Moriggi
E
E
Napoletano
M
M
Regazzoni
C
C
Manfredini
S
S
Mercurio
T P
TP
Pellacini
F
F
D000606:Amino Sugars / Q000737:chemistry*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000627:therapeutic use*; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004487:Edema / Q000188:drug therapy* / Q000473:pathology; D004917:Erythromycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D051379:Mice
D000606:Amino Sugars; D000893:Anti-Inflammatory Agents; C110125:desosamine; D004917:Erythromycin