15-amido erythromycins: synthesis and in vitro activity of a new class of macrolide antibiotics.
An array of 15-amido substituted erythromycin A compounds was synthesized using a chemobiosynthesis approach. It was found that while the in vitro antibacterial activities of aryl amides were inferior to erythromycin A, substituted benzylamides showed equivalent and in some cases improved activity against the macrolide-resistant strains. The 15-amidoerythromycins represent a new class of antibacterial macrolides.
Shaw
Simon J
SJ
Kosan Biosciences, Inc., 3832, Bay Center Place, Hayward, California 94545, USA. shaw@kosan.com
Abbanat
Darren
D
Ashley
Gary W
GW
Bush
Karen
K
Foleno
Barbara
B
Macielag
Mark
M
Zhang
Dan
D
Myles
David C
DC
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004917:Erythromycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006193:Haemophilus influenzae / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D021241:Spectrometry, Mass, Electrospray Ionization; D013296:Streptococcus pneumoniae / Q000187:drug effects; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D004917:Erythromycin