Studies on biologically Active Haloganenated Compounds. III. Synthesis and Antibacterial Activity of 7-Fluoromethyl-1, 8-naphthyridine and Quinoline Derivatives

Abstract

Some novel compounds having a fluoromethyl group at the C₇-position on 1-alkyl-1, 4-dihydro-4-oxo-1, 8-naphthyridine-3-carboxylic acid and on 1-alkyl-1, 4-dihydro-4-oxo-quinoline-3-carboxylic acid were prepared and their antibacterial activities were examined in vitro. In a series of quinolines, no striking difference of antibacterial activities between the 7-fluoromethyl and 7-methyl derivatives was observed. However, the activity was increased in the series of 1, 8-naphthyridines by replacement of the methyl group with the fluoromethyl group. As regards the N₁-substituents, the 2-fluoroethyl compound showed a higher activity than the others.