Synthesis of novel 5-fluoro analogs of norfloxacin and ciprofloxacin

DB Moran, CB Ziegler Jr, TS Dunne…

Index: Moran; Ziegler Jr.; Dunne; Kuck; Lin Journal of Medicinal Chemistry, 1989 ,  vol. 32,  # 6  p. 1313 - 1318

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Citation Number: 34

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-tetratluoroquinolone 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- ...