Synthesis and antibacterial activity of 4″,11-di-O-arylalkylcarbamoyl azithromycin derivatives

作者: Shutao Ma , Bo Jiao , Zhaopeng Liu , Hui Wang , Ruiqing Xian

DOI: 10.1016/J.BMCL.2009.01.092

关键词: MicrobiologyAntibacterial activityChemistryBacteriaAntibacterial agentChemical synthesisStreptococcaceaeBiological activityStreptococcus pneumoniaeStereochemistryAzithromycinOrganic chemistryClinical biochemistryMolecular medicineBiochemistryMolecular biologyDrug discoveryPharmaceutical Science

摘要: Abstract A series of new 4″,11-di-O-arylalkylcarbamoyl azithromycin derivatives were designed, synthesized and evaluated for their in vitro antibacterial activities. Some exhibited greatly improved activity against erythromycin-resistant bacteria. Among them, compounds 5f 5k found to have potent Streptococcus pneumoniae whose resistance was encoded by the erm or mef gene.

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