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Synthesis and antibacterial activity of novel 4''-O-arylalkylcarbamoyl and 4''-O-((arylalkylamino)-4-oxo-butyl)carbamoyl clarithromycin derivatives.

Bioorganic & medicinal chemistry letters (2010-05-14)
Yongjing Ju, Ruiqing Xian, Ling Zhang, Ruixin Ma, Jichao Cao, Shutao Ma
ABSTRACT

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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Erythromycin, meets USP testing specifications
Sigma-Aldrich
Erythromycin, potency: ≥850 μg per mg
Sigma-Aldrich
Erythromycin, tested according to Ph. Eur.
Sigma-Aldrich
Erythromycin, BioReagent, suitable for cell culture