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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).

作者信息

Morita S, Otsubo K, Uchida M, Kawabata S, Tamaoka H, Shimizu T

机构信息

Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd., Japan.

出版信息

Chem Pharm Bull (Tokyo). 1990 Jul;38(7):2027-9. doi: 10.1248/cpb.38.2027.

DOI:10.1248/cpb.38.2027
PMID:2268907
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.

摘要

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