Synthesis and in vitro antibacterial activity of 7-(4-alkoxyimino-3-methyl-3-methylaminopiperidin-1-yl)quinolones / 药学学报
Acta Pharmaceutica Sinica
; (12): 860-8, 2010.
Article
in English
| WPRIM (Western Pacific)
| ID: wpr-382456
Responsible library:
WPRO
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.
Full text:
Available
Database:
WPRIM (Western Pacific)
Language:
English
Journal:
Acta Pharmaceutica Sinica
Year:
2010
Document type:
Article