NOVEL PYRIDONECARBOXYLIC ACID DERIVATIVES OR SALTS THEREOF AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT

摘要

PURPOSE: Provided are novel pyridonecarboxylic acid derivatives or salts thereof which exhibit excellent antibacterial activities and peroral absorbability, and medicines comprising such a compound as an active ingredient. CONSTITUTION: Pyridonecarboxylic acid derivatives are represented by the general formula (1): wherein R¬1 is -OH, a carboxy-protecting group or (alkyl)-amino group, R¬2 is H, or -NO2, (protected) amino, (protected) hydroxyl, lower alkyl or lower alkoxyl group, R¬3 is a halogen atom, H, or -NO2, lower alkyl, lower alkoxyl or amino group, R¬4 is an azido, (substituted) hydrazino, (substituted) amino, lower alkoxyl or hydroxyl group, R¬5, R¬6 and R¬7 are independently H, -NO2, halogen atom or lower alkyl group, R¬8 is a -NO2, (substituted) amino, -OH or lower alkoxyl group, A is N or C-R¬12, in which R¬12 is H, halogen atom, or (substituted) lower alkyl, lower alkenyl, lower alkynyl, lower alkoxyl, lower alkylthio or nitro group, and B is N or C-R¬13, in which R¬13 is H or halogen atom, or salts thereof, and medicine comprising such a compound as an active ingredient. The derivatives or the salts thereof exhibit excellent antibacterial action and peroral absorbability, scarcely cause side effects, and are easy of synthesis.