PYRIDONECARBOXYLIC ACIDS AS ANTIBACTERIAL AGENTS .8. SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIP OF OCYCLOPROPYL)-4-OXO-1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACIDS AND 7-(1-AMINOCYCLOPROPYL)-4-OXOQUINOLINE-3-CARBOXYLIC ACIDS

4-Oxo-1,8-naphthyridine- and 4-oxoquinoline-3-carboxylic acids (2a,b a nd 3a-1) possessing a 1-aminocyclopropyl group at the 7-position have been synthesized and evaluated for in vitro antibacterial activities. The three quinolones (3d,h,i) exhibited potent antibacterial activitie s against both gram-positive and gram-negative bacteria, which are com parable to those of ciprofloxacin (CPFX) and ofloxacin (OFLX). Among t he three compounds, the best pharmacological and pharmacokinetic profi le was obtained with 3i, an OFLX analogue, which was considerably less toxic than three reference quinolones (1, CPFX, and OFLX).