Ishikawa H, Tabusa F, Miyamoto H, Kano M, Ueda H, Tamaoka H, Nakagawa K
Chem Pharm Bull (Tokyo). 1989 Aug;37(8):2103-8. doi: 10.1248/cpb.37.2103.
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.
合成了一系列取代的6,7-二氢-1-氧代-1H,5H-苯并[i,j]喹嗪-2-羧酸，并对其抗菌活性进行了测试。其中，9-氟-6,7-二氢-5-甲基-8-(4-甲基-1-哌嗪基)-1-氧代-1H,5H-苯并[i,j]喹嗪-2-羧酸（OPC-7241）对革兰氏阳性菌和阴性菌表现出强效抗菌活性，包括金黄色葡萄球菌和铜绿假单胞菌，而9-氟-6,7-二氢-8-(4-羟基-1-哌啶基)-5-甲基-1-氧代-1H,5H-苯并[i,j]喹嗪-2-羧酸（OPC-7251）对痤疮丙酸杆菌表现出特征性的强效活性。
