title: Synthesis and antibacterial activity of 4''-O-heteroarylcarbamoyl derivatives of macrolide.
abstract: A series of novel 4''-position modified macrolide derivatives has been synthesized via a facile procedure. Their in vitro antibacterial activities against constitutively erythromycin-resistant strains were evaluated. Among the derivatives tested, compound 8a which has 11,12-carbamate and 4''-O-heteroarylcarbamoyl groups was found to have potent activity against most resistant bacteria.
authors.affiliation: Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, China.
authors.forename: Peng
authors.initials: P
authors.lastname: Xu
authors.forename: Lu
authors.initials: L
authors.lastname: Liu
authors.forename: Zhi-ping
authors.initials: ZP
authors.lastname: Jin
authors.forename: Guang-qiang
authors.initials: GQ
authors.lastname: Wang
authors.forename: Jian
authors.initials: J
authors.lastname: Liu
authors.forename: Yun
authors.initials: Y
authors.lastname: Li
authors.forename: Ping-sheng
authors.initials: PS
authors.lastname: Lei
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry*; D002219:Carbamates / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D017291:Clarithromycin / Q000737:chemistry*; D018360:Crystallography, X-Ray / Q000379:methods; D015195:Drug Design; D013293:Enterococcus faecalis / Q000378:metabolism; D004917:Erythromycin / Q000138:chemical synthesis* / Q000494:pharmacology; D018942:Macrolides / Q000138:chemical synthesis* / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D008956:Models, Chemical; D011500:Protein Synthesis Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D002219:Carbamates; D018942:Macrolides; D011500:Protein Synthesis Inhibitors; D004917:Erythromycin; D017291:Clarithromycin