Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships

K Araki, T Kuroda, S Uemori, A Moriguchi…

Index: Araki; Kuroda; Uemori; Moriguchi; Ikeda; Hirayama; Yokoyama; Iwao; Yakushiji Journal of Medicinal Chemistry, 1993 , vol. 36, # 10 p. 1356 - 1363

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Citation Number: 25

Abstract

A series of novel 7-substituted l-cyclopropyl-6, 8-difluoro-l, 4-dihydro-4-oxo-3- quinolinecarboxylic acids have been prepared and tested for antibacterial activities and for convulsive activities in combination with nonsteroidal antiinflammatory drug. Structure- activity relationships revealed that 7-(2-(aminomethyl) marpholino) derivative 28 had a better Gram-positive activity than the reference quinolones, such as ciprofloxacin, ...