title: Synthesis and antibacterial activity of C12 des-methyl ketolides.
abstract: Synthesis of C(12) des-methyl ketolide is developed featuring an intramolecular epoxide formation/elimination process to establish the C(12) stereocenter. These ketolides are potent against several key respiratory pathogens, including erythromycin resistant erm- and mef-containing strains of Streptococcus pneumoniae.
authors.affiliation: Small Molecule Drug Discovery, Biopharma Research, Chiron Corporation, Emeryville, CA 94608, USA. xiaodong_lin@chiron.com
authors.forename: Xiaodong
authors.initials: X
authors.lastname: Lin
authors.forename: Alice C
authors.initials: AC
authors.lastname: Rico
authors.forename: Daniel T
authors.initials: DT
authors.lastname: Chu
authors.forename: Georgia L
authors.initials: GL
authors.lastname: Carroll
authors.forename: Lynn
authors.initials: L
authors.lastname: Barker
authors.forename: Ribhi
authors.initials: R
authors.lastname: Shawar
authors.forename: Manoj C
authors.initials: MC
authors.lastname: Desai
authors.forename: Jacob J
authors.initials: JJ
authors.lastname: Plattner
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002244:Carbon / Q000737:chemistry*; D006095:Gram-Positive Cocci / Q000187:drug effects; D006193:Haemophilus influenzae / Q000187:drug effects; D048628:Ketolides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008745:Methylation; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D048628:Ketolides; D002244:Carbon