title: Synthesis and antibacterial activity of the metabolites of 9-fluoro-6,7-dihydro-8-(4-hydroxy-1-piperidyl)-5-methyl-1-oxo-1H,5H- benzo[i,j]quinolizine-2-carboxylic acid (OPC-7251).
abstract: The metabolites of 9-fluoro-6,7-dihydro-8-(4-hydroxy-1-piperidyl)-5-methyl-1-oxo-1H,5H- benzo[i,j]quinolizine-2-carboxylic acid (OPC-7251) (1), which has a potent antibacterial activity against gram-positive bacteria, characteristically Propionibacterium acnes, were synthesized to confirm their structures and to examine their antibacterial activity. The structures of three major metabolites (2, 3a and 4) were identified by means of comparison with the synthetic compounds. The antibacterial activity of the metabolites (2, 3a and 4) was found to be lower than that of 1.
authors: Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd., Japan.
authors: S
authors: S
authors: Morita
authors: K
authors: K
authors: Otsubo
authors: M
authors: M
authors: Uchida
authors: S
authors: S
authors: Kawabata
authors: H
authors: H
authors: Tamaoka
authors: T
authors: T
authors: Shimizu
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis*; D001419:Bacteria / Q000187:drug effects*; D024841:Fluoroquinolones; D008826:Microbial Sensitivity Tests; D011807:Quinolizines / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones; D011807:Quinolizines; C062127:nadifloxacin