4-OXOQUINOLIZINE ANTIMICROBIALS HAVING 2-PYRIDONE SKELETON AS PARTIAL STRUCTURE

摘要

4-Oxoquinolizine derivatives (I) are new. 4-Oxoquinolizine derivatives of formula (I) and their salts are new. [Image] R1>H or carboxy protecting group; R2>H, halo, lower alkyl, lower alkoxy or OH; R3>phenyl or Het both optionally substituted by lower alkyl, lower alkoxy, NO2, CN, NH2, acyl, CONH2, ureido, halo, OH, or COOH; Het : 5 or 6 membered aromatic heterocyclyl; and R4>H or halo. ACTIVITY : Antibacterial. In assays 8-(4-aminophenyl)-1-cyclopropyl-9-methyl-4-oxo-4H-quinolizine-3-carboxylic acid had the following MIC (Microg/ml) values: Staphyloccocus aureus IFO 13276 (less than or equal to 0.004), Staphyloccocus aureus Clin-211 (0.031) and Escherichia coli IFO 12734 (0.063). The corresponding values for levoxacin were 0.125, 4 and 0.031 Microg/ml, respectively. MECHANISM OF ACTION : None given.