Synthesis and antibacterial activity of 4'',11-di-O-arylalkylcarbamoyl azithromycin derivatives.
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.
Ma
Shutao
S
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, Jinan 250012, PR China.
Jiao
Bo
B
Liu
Zhaopeng
Z
Wang
Hui
H
Xian
Ruiqing
R
Zheng
Manjie
M
Lou
Hongxiang
H
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
D000900:Anti-Bacterial Agents; D001426:Bacterial Proteins; D018942:Macrolides; C117866:MefA protein, Streptococcus; D008565:Membrane Proteins; D017963:Azithromycin; D008780:Methyltransferases; C431709:ErmA protein, Bacteria