title: Synthesis and antibacterial activity of 6-O-heteroarylcarbamoyl-11,12-lactoketolides.
abstract: 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.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 1000 Route 202, PO Box 300, Raritan, NJ 08869, USA. egrant@prdus.jnj.com
authors.forename: Eugene B
authors.initials: EB
authors.lastname: Grant
authors.forename: Deodialsingh
authors.initials: D
authors.lastname: Guiadeen
authors.forename: Darren
authors.initials: D
authors.lastname: Abbanat
authors.forename: Barbara D
authors.initials: BD
authors.lastname: Foleno
authors.forename: Karen
authors.initials: K
authors.lastname: Bush
authors.forename: Mark J
authors.initials: MJ
authors.lastname: Macielag
mesh_terms: 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
chemical_list: D000900:Anti-Bacterial Agents; D048628:Ketolides