Design, synthesis and in vitro antibacterial activity of 7-(4-alkoxyimino-3-aminomethylpiperidin-1-yl)fluoroquinolone derivatives
| Autor: | Yun Chai, Hong Yi, Lan-Ying Sun, Jian Wang, Huiyuan Guo, Xuefu You, Mingliang Liu |
|---|---|
| Rok vydání: | 2011 |
| Předmět: |
Gemifloxacin
Clinical Biochemistry Pharmaceutical Science Microbial Sensitivity Tests medicine.disease_cause Biochemistry Chemical synthesis Levofloxacin Drug Discovery medicine Molecular Biology Antibacterial agent Molecular Structure Chemistry Pseudomonas aeruginosa Organic Chemistry Biological activity Combinatorial chemistry Anti-Bacterial Agents Ciprofloxacin Drug Design Molecular Medicine Antibacterial activity medicine.drug Fluoroquinolones Imino Pyranoses |
| Zdroj: | Bioorganicmedicinal chemistry letters. 21(11) |
| ISSN: | 1464-3405 |
| Popis: | We report herein the design and synthesis of novel 7-(4-alkoxyimino-3-aminomethylpiperidin-1-yl) fluoroquinolone derivatives. The antibacterial activity of the newly synthesized compounds was evaluated and compared with gemifloxacin, levofloxacin and ciprofloxacin. Results reveal that compounds 10 , 16 , and 17 have good activity against all of the tested Gram-positive organisms including drug-resistance strains (MICs: 0.125–4 μg/mL). In addition, compounds 16 and 17 (MICs: 4 μg/mL) were 2- to 8-fold more potent than the reference drugs against Pseudomonas aeruginosa. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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