Studies on antibacterial agents. II. Synthesis and antibacterial activities of substituted 1,2-dihydro-6-oxo-6H-pyrrolo[3,2,1-ij]quinoline-5-carboxylic acids |
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| Authors: | H Ishikawa T Uno H Miyamoto H Ueda H Tamaoka M Tominaga K Nakagawa |
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| Institution: | 2nd Tokushima Institute of New Drugs Research, Otsuka Pharmaceutical Co., Ltd., Japan. |
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| Abstract: | A series of substituted 1,2-dihydro-6-oxo-pyrrolo3,2,1-ij]quinoline-5-carboxylic acids for the treatment of systemic infections was synthesized via 7-bromo-3-ethylthio-4,5-difluoro-2-methylindole (3), which was prepared by Gassman's indole synthesis in excellent yield. The synthesized pyrroloquinolines were tested for their antibacterial activities. 8-Fluoro-1,2-dihydro-2-methyl-9-(4-methyl-1-piperazinyl)-6-oxo-6H- pyrrolo3,2,1-ij]quinoline-5-carboxylic acid showed a potent antibacterial activity against gram-positive and gram-negative bacteria. |
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