Synthesis and Structure-Activity Relationship of 1-Aryl-6,8-difluoroquinolone Antibacterial Agents

Article abstract of DOI:10.1021/jm00386a011

A series of new arylfluoroquinolones has been prepared.These derivatives are characterized by having fluorine atoms at the 6- and 8-positions, substituted amino groups at the 7-position, and substituted phenyl groups at the 1-position.The in vitro antibacterial potency is greatest when the 1-substituent is 2,4-difluorophenyl and the 7-substituent is a 3-amino-1-pyrrolidinyl group. 1-(4-Fluorophenyl)-6,8-difluoro-7-piperazin-1-yl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid (22) was found to possesss excellent in vitro potency and in vivo efficacy.