Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds
| Autor: | Lan-Ying Sun, Zengquan Wei, Lian-Shun Feng, Kai Lv, Mingliang Liu, Hui-Quan Guo, Yexin Sun |
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| Rok vydání: | 2011 |
| Předmět: |
Drug
Male Pyrrolidines Stereochemistry Gemifloxacin media_common.quotation_subject medicine.disease_cause Pyrrolidine chemistry.chemical_compound Mice Drug Discovery Oximes medicine Animals Naphthyridines Pathogen media_common Pharmacology Bacteria Pseudomonas aeruginosa Organic Chemistry General Medicine Anti-Bacterial Agents Ciprofloxacin chemistry Antibacterial activity medicine.drug |
| Zdroj: | European journal of medicinal chemistry. 47(1) |
| ISSN: | 1768-3254 |
| Popis: | A series of novel naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds were designed and synthesized. These derivatives were initially evaluated for their in vitro antibacterial activity and compounds 13a1, b1 were chosen for further evaluation their in vivo activity against systemic infections in mice. The results indicate that all of the target compounds have considerable in vitro antibacterial activity. In the in vivo experiments, 13b1 was found to be more effective than the parent drug gemifloxacin against the tested five strains, and especially its activity (ED 50 :21.27 mg/kg) is 5.2–6.1 times more potent than gemifloxacin and ciprofloxacin against clinically important Gram-negative pathogen Pseudomonas aeruginosa . |
| Databáze: | OpenAIRE |
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