title: Synthesis of antimicrobial agents. 1. Syntheses and antibacterial activities of 7-(azole substituted)quinolones.
abstract: A series of 6-fluoro- and 6,8-difluoro-7-(azole substituted)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids were prepared. Structure-activity relationship studies indicated that the antibacterial potency was better when the 6,8-substituents were fluorine atoms and the 7-substituent was either 1-imidazolyl, 20, or 4-methyl-1-imidazolyl, 25. From the results of studies on pharmacokinetic profile and toxicity, 20 and 25 were found to possess excellent antibacterial activities and to show high blood levels after oral administration to mice with low toxicity.
authors: Pharmaceuticals Research Center, Kanebo Ltd., Osaka, Japan.
authors: T
authors: T
authors: Uno
authors: M
authors: M
authors: Takamatsu
authors: Y
authors: Y
authors: Inoue
authors: Y
authors: Y
authors: Kawahata
authors: K
authors: K
authors: Iuchi
authors: G
authors: G
authors: Tsukamoto
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000097:blood / Q000138:chemical synthesis* / Q000494:pharmacology; D001393:Azoles / Q000097:blood / Q000138:chemical synthesis* / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects*; D008297:Male; D051379:Mice; D011804:Quinolines / Q000097:blood / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D001393:Azoles; D011804:Quinolines