title: Synthesis and antibacterial activity of 3-O-acyl-6-O-carbamoyl erythromycin A derivatives.
abstract: A series of 3-O-acyl-6-O-carbamoyl erythromycin A derivatives has been synthesized. Several functional groups were identified as the optimal C3-substituents, and the best compounds in this series possess potent in vitro antibacterial activity against erythromycin-susceptible and erythromycin-resistant bacteria.
authors.affiliation: Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, L.L.C. 1000 Route 202, PO Box 300, Raritan, NJ 08869, USA. bzhu@prdus.jnj.com
authors.forename: Bin
authors.initials: B
authors.lastname: Zhu
authors.forename: Brett A
authors.initials: BA
authors.lastname: Marinelli
authors.forename: Darren
authors.initials: D
authors.lastname: Abbanat
authors.forename: Barbara D
authors.initials: BD
authors.lastname: Foleno
authors.forename: Todd C
authors.initials: TC
authors.lastname: Henninger
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 / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects*; D004917:Erythromycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D048628:Ketolides / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D048628:Ketolides; D004917:Erythromycin; C106791:telithromycin