Document Report Card

ID: ALA1124495

Journal: J Med Chem

Title: Synthesis of novel 5-fluoro analogues of norfloxacin and ciprofloxacin.

Authors: Moran DB, Ziegler CB, Dunne TS, Kuck NA, Lin YI.

Abstract: A series of polyfluoro-3-quinolonecarboxylic acids have been synthesized and their in vitro antibacterial activity evaluated. The desired 7-(substituted amino) derivatives were prepared from the 5,6,7,8-tetrafluoroquinolone acids. Conversely, amine displacement occurred primarily at the 5-position when the ester was used. Structure-activity studies indicated that the antibacterial activity was greatest when the N-1 substituent was cyclopropyl and the 7-substituent was 4-methyl-1-piperazinyl. All 5-(substituted amino) derivatives showed poor in vitro activity.

CiteXplore: 2498519

DOI: 10.1021/jm00126a028