Synthesis and in vitro antibacterial activity of 7-(3-Alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives
| Autor: | Su-Jie Li, Yun Chai, Mingliang Liu, Yi-Bin Zhang, Huiyuan Guo, Bo Wang, Juxian Wang |
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| Rok vydání: | 2011 |
| Předmět: |
Models
Molecular Cell Survival Gemifloxacin Staphylococcus Drug Evaluation Preclinical Microbial Sensitivity Tests Crystallography X-Ray medicine.disease_cause Enterococcus faecalis Cell Line Microbiology Structure-Activity Relationship Dogs Staphylococcus epidermidis Drug Discovery Streptococcus pneumoniae medicine Animals Antibacterial agent Pharmacology Bacteria Dose-Response Relationship Drug Molecular Structure biology Chemistry Organic Chemistry Stereoisomerism General Medicine biology.organism_classification Gatifloxacin Anti-Bacterial Agents Staphylococcus aureus Drug Design Antibacterial activity Fluoroquinolones medicine.drug |
| Zdroj: | European Journal of Medicinal Chemistry. 46:2421-2426 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2011.03.026 |
| Popis: | A series of novel 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl)fluoroquinolone derivatives were designed, synthesized and evaluated for their in vitro antibacterial activity and cytotoxicity. All of the target compounds have potent antibacterial activity against the tested Gram-positive and Gram-negative strains, and exhibit good potency in inhibiting the growth of Staphylococcus aureus including MRSA, Staphylococcus epidermidis including MRSE and Streptococcus pneumoniae (MICs: 0.125-4 μg/mL). Compound 22, with the best activity against Gram-positive strains, is 4-16 fold more potent than gemifloxacin, gatifloxacin and levofloxacin against Enterococcus faecalis, and 16- and 4-fold more potent than levofloxacin against S. epidermidis 09-6 and S. pneumoniae 08-4, respectively. |
| Databáze: | OpenAIRE |
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