Studies on Antibacterial Agents. I. : Synthesis of Substituted 6, 7-Dihydro-1-oxo-1H, 5H, -benzo{i, j]-quinolizine-2-carboxylic Acids

Hiroshi ISHIKAWA; Fujio TABUSA; Hisashi MIYAMOTO; Masanobu KANO; Hiraki UEDA; Hisashi TAMAOKA; Kazuyuki NAKAGAWA

doi:10.1248/cpb.37.2103

Hiroshi ISHIKAWA, Fujio TABUSA, Hisashi MIYAMOTO, Masanobu KANO, Hiraki UEDA, Hisashi TAMAOKA, Kazuyuki NAKAGAWA

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Keywords: 4-oxoquinoline-3-carboxylic acid, benzo[i, j]quinolizine, tetrahydroquinoline, N-methylpiperazine, 4-hydroxypiperidine, Propionibacterium acnes, antibacterial activity

JOURNAL FREE ACCESS

1989 Volume 37 Issue 8 Pages 2103-2108

DOI https://doi.org/10.1248/cpb.37.2103

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Abstract

A series of substituted 6, 7-dihydro-1-oxo-1H, 5H-benzo[i, j]quinolizine-2-carboxylic acids was synthesized and tested for antibacterial activities. Among them, 9-fluoro-6, 7-dihydro-5-methyl-8-(4-methyl-1-piperazinyl)-1-oxo-1H, 5H-benzo[i, j]quinolizine-2-carboxylic acid (OPC-7241) exhibited potent antibacterial activity against gram-positive and -negative bacteria, including Staphylococcus aureus and Pseudomonas aeruginosa, and 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) showed potent activity characteristically against Propionibacterium acnes.

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