896709-65-2Relevant academic research and scientific papers
Synthesis and antibacterial evaluation of novel clarithromycin derivatives with C-4″ elongated arylalkyl groups against macrolide-resistant strains
Ma, Shutao,Jiao, Bo,Ju, Yongjing,Zheng, Manjie,Ma, Ruixin,Liu, Lin,Zhang, Ling,Shen, Xuecui,Ma, Chenchen,Meng, Ya,Wang, Hui,Qi, Yunkun,Ma, Xiaodong,Cui, Wenping
supporting information; experimental part, p. 556 - 566 (2011/03/20)
Novel clarithromycin derivatives with C-4″ elongated arylalkyl groups were designed, synthesized and evaluated to probe the effect of different lengths of their C-4″ side chains on the activity against resistant bacterial strains. These derivatives had excellent activity against erythromycin-susceptible Streptococcus pneumoniae, Streptococcus aureus or Streptococcus pyogenes and some of them exhibited greatly improved activity against erythromycin-resistant strains. Compounds 18 and 16, which had the C-4″ elongated arylalkyl groups with eight atoms from the 4″-oxygen atom to the terminal benzene ring, were the most effective against S. pneumoniae expressing the erm gene and the erm and mef genes. In contrast, the most potent compounds 3, 5, 9, 17 and 18 against S. pneumoniae expressing the mef gene had C-4″ elongated arylalkyl groups with three to eight atoms between the 4″-oxygen atom and the terminal aromatic ring.
Synthesis and antibacterial activity of novel 4″-O-arylalkylcarbamoyl and 4″-O-((arylalkylamino)-4-oxo-butyl)carbamoyl clarithromycin derivatives
Ju, Yongjing,Xian, Ruiqing,Zhang, Ling,Ma, Ruixin,Cao, Jichao,Ma, Shutao
supporting information; experimental part, p. 3272 - 3274 (2010/08/06)
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 μg/mL) against Streptococcus pneumonia encoded by the erm gene and compound 4a was had the most potent activity (0.25 μg/mL) against S. pneumonia encoded by the erm and mef genes.
