Synthesis and antibacterial activity of new 7-(aminoazabicycloalkanyl)quinolonecarboxylic acids
A series of novel 7--6-fluoro-1-substituted quinolinecarboxylic acids (18-53) have been prepared and their antibacterial activities evaluated.These compounds are characterized structurally by a new amino-substituted azabicyclooctane, -nonane and -decane ring systems at the 7-position of quinolonecarboxylic acids.To compare the biological activities of enantiomers, (+)-7-octan-3-yl>-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolonecarboxylicacid hydrochloride (43, 44) were synthesized and evaluated for antibacterial activity.Compound 43 was more potent than 44 against both Gram-positive and Gram-negative organisms.The structure-activity relationships of these quinolonecarboxylic acids are also discussed. antibacterial activity / amino-substituted azabicycloalkane ring / substituted quinolonecarboxylic acids / structure-activity relationships