Synthesis and antibacterial activity of N-[2-[5-(methylthio)thiophen-2- yl]-2-oxoethyl] and N-[2-[5-(methylthio)thiophen-2-yl]-2-(oxyimino)ethyl]pip derivatives
A number of N-substituted piperazinylquinolone derivatives were synthesized and evaluated for antibacterial activity against Gram-positive and Gram-negative bacteria. Preliminary results indicated that most compounds tested in this study demonstrated comparable or better activity against Staphylococ...
Saved in:
Published in | Bioorganic & medicinal chemistry Vol. 14; no. 10; pp. 3421 - 3427 |
---|---|
Main Authors | , , , , , , |
Format | Journal Article |
Language | English |
Published |
01.01.2006
|
Subjects | |
Online Access | Get full text |
Cover
Loading…
Summary: | A number of N-substituted piperazinylquinolone derivatives were synthesized and evaluated for antibacterial activity against Gram-positive and Gram-negative bacteria. Preliminary results indicated that most compounds tested in this study demonstrated comparable or better activity against Staphylococcus aureus and Staphylococcus epidermidis than their parent piperazinylquinolones as reference drugs. Among these derivatives, ciprofloxacin derivative 5a, containing N-[2-[5-(methylthio)thiophen-2-yl]-2-oxoethyl] residue, showed significant improvement of potency against staphylococci, maintaining Gram-negative coverage. |
---|---|
Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 content type line 23 ObjectType-Feature-2 |
ISSN: | 0968-0896 1464-3391 |
DOI: | 10.1016/j.bmc.2005.12.058 |