Synthesis and antibacterial activity of novel 4''-O-arylalkylcarbamoyl and 4''-O-((arylalkylamino)-4-oxo-butyl)carbamoyl clarithromycin derivatives.
Novel series of novel 4''-O-arylalkylcarbamoyl and 4''-O-((arylalkylamino)-4-oxo-butyl)carbamoyl clarithromycin derivatives were designed, synthesized and evaluated for their in vitro antibacterial activities. These derivatives retained excellent activity against the erythromycin-susceptible strains and showed significantly improved activity against all of the tested erythromycin-resistant strains. Among them, compound 4c was the most effective (0.06 microg/mL) against Streptococcus pneumonia encoded by the erm gene and compound 4a was had the most potent activity (0.25 microg/mL) against S. pneumonia encoded by the erm and mef genes.
Ju
Yongjing
Y
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, Jinan 250012, PR China.
Xian
Ruiqing
R
Zhang
Ling
L
Ma
Ruixin
R
Cao
Jichao
J
Ma
Shutao
S
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017291:Clarithromycin / Q000031:analogs & derivatives*; D005798:Genes, Bacterial; D008826:Microbial Sensitivity Tests; D013296:Streptococcus pneumoniae / Q000187:drug effects* / Q000235:genetics
D000900:Anti-Bacterial Agents; D017291:Clarithromycin