title: Synthesis and antibacterial activity of novel modified 5-O-mycaminose 14-membered ketolides.
abstract: A practicable method of introducing a side chain to the C-4' position of 5-O-desosamine in the 14-membered ketolides was developed. And using this method, a series of novel modified 5-O-mycaminose ketolides were synthesized. These ketolides containing 5-O-4'-carbamate mycaminose were evaluated for their in vitro antibacterial activities against some respiratory pathogens. 15b and 18e showed comparable activity to telithromycin and clarithromycin.
authors.affiliation: State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Beijing Key Laboratory of Active Substances Discovery and Drugability Evaluation, Department of Medicinal Chemistry, Institute of Materia Medica, Peking Union Medical College, Chinese Academy of Medical Sciences, Beijing 100050, PR China.
authors.forename: Yanpeng
authors.initials: Y
authors.lastname: Xu
authors.forename: Xiaozhuo
authors.initials: X
authors.lastname: Chen
authors.forename: Di
authors.initials: D
authors.lastname: Zhu
authors.forename: Yi
authors.initials: Y
authors.lastname: Liu
authors.forename: Zhehui
authors.initials: Z
authors.lastname: Zhao
authors.forename: Longlong
authors.initials: L
authors.lastname: Jin
authors.forename: Chao
authors.initials: C
authors.lastname: Liu
authors.forename: Pingsheng
authors.initials: P
authors.lastname: Lei
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004352:Drug Resistance, Microbial / Q000187:drug effects; D048628:Ketolides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008712:Methicillin / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013211:Staphylococcus aureus / Q000187:drug effects*; D013212:Staphylococcus epidermidis / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D048628:Ketolides; D008712:Methicillin
keywords: 14-Membered ketolide; Antibacterial activity; Desosamine; Mycaminose; Synthesis