title: Synthesis and antibacterial activity of 4'',11-di-O-arylalkylcarbamoyl azithromycin derivatives.
abstract: A series of new 4'',11-di-O-arylalkylcarbamoyl azithromycin derivatives were designed, synthesized and evaluated for their in vitro antibacterial activities. Some derivatives exhibited greatly improved activity against erythromycin-resistant bacteria. Among them, compounds 5f and 5k were found to have potent activity against erythromycin-resistant Streptococcus pneumoniae whose resistance was encoded by the erm or mef gene.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, Jinan 250012, PR China.
authors.forename: Shutao
authors.initials: S
authors.lastname: Ma
authors.forename: Bo
authors.initials: B
authors.lastname: Jiao
authors.forename: Zhaopeng
authors.initials: Z
authors.lastname: Liu
authors.forename: Hui
authors.initials: H
authors.lastname: Wang
authors.forename: Ruiqing
authors.initials: R
authors.lastname: Xian
authors.forename: Manjie
authors.initials: M
authors.lastname: Zheng
authors.forename: Hongxiang
authors.initials: H
authors.lastname: Lou
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D017963:Azithromycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D001426:Bacterial Proteins / Q000235:genetics; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D024901:Drug Resistance, Multiple, Bacterial / Q000187:drug effects / Q000235:genetics; D018942:Macrolides / Q000737:chemistry; D008565:Membrane Proteins / Q000235:genetics; D008780:Methyltransferases / Q000235:genetics; D008826:Microbial Sensitivity Tests; D008956:Models, Chemical; D013290:Streptococcal Infections / Q000235:genetics / Q000517:prevention & control; D013296:Streptococcus pneumoniae / Q000378:metabolism
chemical_list: D000900:Anti-Bacterial Agents; D001426:Bacterial Proteins; D018942:Macrolides; C117866:MefA protein, Streptococcus; D008565:Membrane Proteins; D017963:Azithromycin; D008780:Methyltransferases; C431709:ErmA protein, Bacteria