title: Synthesis and antibacterial activity of C-6 carbamate ketolides, a novel series of orally active ketolide antibiotics.
abstract: A new series of antibacterial ketolides is reported, which features the use of a C-6 carbamate for tethering the arylalkyl sidechain to the macrolide core. The best members of this series display in vitro and in vivo activity comparable to telithromycin. Partial epimerization at C-2, unobserved in previously reported ketolides, was noted for this series.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development, LLC, 1000 Route 202, PO Box 300, Raritan, NJ 08869, USA. thenning@prdus.jnj.com
authors.forename: Todd C
authors.initials: TC
authors.lastname: Henninger
authors.forename: Xiaodong
authors.initials: X
authors.lastname: Xu
authors.forename: Darren
authors.initials: D
authors.lastname: Abbanat
authors.forename: Ellen Z
authors.initials: EZ
authors.lastname: Baum
authors.forename: Barbara D
authors.initials: BD
authors.lastname: Foleno
authors.forename: Jamese J
authors.initials: JJ
authors.lastname: Hilliard
authors.forename: Karen
authors.initials: K
authors.lastname: Bush
authors.forename: Dennis J
authors.initials: DJ
authors.lastname: Hlasta
authors.forename: Mark J
authors.initials: MJ
authors.lastname: Macielag
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000138:chemical synthesis*; D002219:Carbamates / Q000008:administration & dosage / Q000138:chemical synthesis*; D005260:Female; D048628:Ketolides / Q000008:administration & dosage / Q000138:chemical synthesis*; D051379:Mice; D008826:Microbial Sensitivity Tests / Q000706:statistics & numerical data
chemical_list: D000900:Anti-Bacterial Agents; D002219:Carbamates; D048628:Ketolides