Synthesis and in vitro antibacterial activity of 7-(4-alkoxyimino-3-methyl-3-methylaminopiperidin-1-yl)quinolones.
- Author:
Zhi-long WAN
1
;
Yun CHAI
;
Ming-liang LIU
;
Hui-yuan GUO
;
Lan-ying SUN
Author Information
1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
- Publication Type:Journal Article
- MeSH:
Anti-Bacterial Agents;
chemical synthesis;
chemistry;
pharmacology;
Gram-Negative Bacteria;
drug effects;
Gram-Positive Bacteria;
drug effects;
Molecular Structure;
Quinolones;
chemical synthesis;
chemistry;
pharmacology
- From:
Acta Pharmaceutica Sinica
2010;45(7):860-868
- CountryChina
- Language:English
-
Abstract:
To explore new agents of quinolone derivatives with high antibacterial activity, 7-(4-alkoxyimino-3-methyl-3-methylaminopiperidin-1-yl)quinolones were designed and synthesized, and their activity against gram-positive and gram-negative strains was tested in vitro. Sixteen target compounds were obtained. Their structures were established by 1H NMR, HRMS and X-ray crystallographic analysis. Compounds 14k and 14m-14o show good antibacterial activity against the tested five gram-positive strains and five gram-negative strains (MIC: 0.25-16 micromg x mL(-1)), of which the most active compound 14o is 8-fold more potent than levofloxacin against S. pneumoniae (MIC: 4 microg x mL(-1)), and comparable to levofloxacin against S. aureus, S. epidermidis, E. faecalis and E. coli (MIC: 0.25-1 microg x mL(-1)), but generally less potent than gemifloxacin.
