Synthesis and antibacterial activity of 6-O-heteroarylcarbamoyl-11,12-lactoketolides.
A new series of erythromycin A derivatives, the 6-O-heteroarylcarbamoyl-11,12-lactoketolides, with activity against macrolide-resistant streptococci, are described. Structurally, these macrolide antibiotics are characterized by a heteroaryl side chain attached to the macrolactone core through a carbamate linkage at the C6 position, as well as 11,12-gamma-lactone and 3-keto functionalities. The synthesis and antibacterial activity of this new series of ketolides are discussed.
Grant
Eugene B
EB
Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 1000 Route 202, PO Box 300, Raritan, NJ 08869, USA. egrant@prdus.jnj.com
Guiadeen
Deodialsingh
D
Abbanat
Darren
D
Foleno
Barbara D
BD
Bush
Karen
K
Macielag
Mark J
MJ
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D006193:Haemophilus influenzae / Q000187:drug effects; D048628:Ketolides / Q000138:chemical synthesis* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D013296:Streptococcus pneumoniae / Q000187:drug effects; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D048628:Ketolides