title: Fluoronaphthyridines and quinolones as antibacterial agents. 1. Synthesis and structure-activity relationships of new 1-substituted derivatives.
abstract: A series of novel 7-piperazinyl-1-substituted-6-fluoroquinolones and naphthyridines have been prepared and their antibacterial activities evaluated. These derivatives are characterized by having alkyl, alkenyl, arylalkyl, cycloalkyl, and cycloalkenyl groups at the 1-position. As a result of this study, derivatives 7 and 26, which are substituted with tert-butyl groups at N-1, were found to possess excellent in vitro and in vivo potency, particularly against Staphylococcus aureus, comparable to that of norfloxacin or ciprofloxacin. Structure-activity relationships of N-1 substituted alkyls and cycloalkyls are also discussed.
authors.affiliation: Centre de Recherche Bristol-Myers, Torcy, France.
authors.forename: D
authors.initials: D
authors.lastname: Bouzard
authors.forename: P
authors.initials: P
authors.lastname: Di Cesare
authors.forename: M
authors.initials: M
authors.lastname: Essiz
authors.forename: J P
authors.initials: JP
authors.lastname: Jacquet
authors.forename: P
authors.initials: P
authors.lastname: Remuzon
authors.forename: A
authors.initials: A
authors.lastname: Weber
authors.forename: T
authors.initials: T
authors.lastname: Oki
authors.forename: M
authors.initials: M
authors.lastname: Masuyoshi
mesh_terms: D042462:4-Quinolones; D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D004285:Dogs; D006090:Gram-Negative Bacteria / Q000187:drug effects; D051379:Mice; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009287:Naphthyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D013210:Staphylococcus / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D042462:4-Quinolones; D000900:Anti-Bacterial Agents; D009287:Naphthyridines