Synthesis and antibacterial activity of 1-(substituted pyrrolyl)-7-(substituted amino)-6-fluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids.
Seventeen quinolone compounds characterized by having a fluorine atom at the 6-position, a substituted amino at the 7-position, and a substituted pyrrolyl at the 1-position were synthesized for the first time. The in vitro antibacterial activities of these compounds against Escherichia coli and Staphylococcus aureus were tested. Among these agents obtained, compound 24 showed significantly enhanced activity against S. aureus. The results indicate that there is much room for modifications at the N-1 position.
Liu
J H
JH
Institute of Medicinal Biotechnology, Chinese Academy of Medical Science, Beijing.
Guo
H Y
HY
D042462:4-Quinolones; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004926:Escherichia coli / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship
D042462:4-Quinolones; D000890:Anti-Infective Agents