Structure-Antibacterial Activity and Cytotoxicity Relationships of Thiazolo and Thiazetoquinolone Derivatives
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概要
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In the course of our search for derivatives with potent antibacterial activity and low cytotoxicity, we have studied the relationships among the structure, antibacterial activity and cytotoxicity of thiazoloquinolone and thiazetoquinolone derivatives (the term quinolone as used in this paper includes the quinolone, 1,8-naphthyridine and pyridopyrimidine nuclei). The antibacterial activities and cytotoxicity of these derivatives were compared with those on norfloxacin, ofloxacin, enoxacin and ciprofloxacin. The antibacterial activities of the thiazoloquinolone derivatives were more potent than those of the dihyrothiazoloquinolone derivatives, and comparable to that of ciprofloxacin. All of the thiazoloquinolone derivatives were highly cytotoxic against mammalian cells, but some of the dihyrothiazoloquinolone derivatives were less cytotoxic, being comparable in cytotoxicity to the reference drugs. The thiazetoquinolone derivatives were less cytotoxic than the thiazoloquinolone derivatives, and one of them, 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid, showed the most potent antibacterial activity of all compounds tested in this study, as well as a very low cytotoxicity. The antibacterial activity and cytotoxicity of this compound were similar to that of ciprofloxacin.
- 公益社団法人日本薬学会の論文
- 1996-11-15
著者
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NISHINO Takeshi
Department of Microbiology, Kyoto Pharmaceutical University
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Nishino Takeshi
Department Of Biochemistry And Molecular Biology Nippon Medical School
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冨井 由文
日本新薬株式会社創薬第二研究所
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Nishino Takeshi
Department Of Microbiology Kyoto Pharmaceutical University
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Matsuoka M
Research Laboratories Nippon Shinyaku Co. Ltd.
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Matsuda Masato
Discovery Research Laboratories Nippon Shinyaku Co. Ltd.
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Kitano M
Research Center Sumitomo Pharmaceuticals Co. Ltd
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SEGAWA Jun
Research Laboratories, Nippon Shinyaku Co., Ltd.,
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OZAKI Masakuni
Discovery Research Laboratories II, Nippon Shinyaku Co., Ltd.,
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SEGAWA Jun
Discovery Research Laboratories II, Nippon Shinyaku Co., Ltd.,
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KITANO Masahiko
Discovery Research Laboratories II, Nippon Shinyaku Co., Ltd.,
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TOMII Yoshifumi
Discovery Research Laboratories II, Nippon Shinyaku Co., Ltd.,
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HONMURA Takuya
Discovery Research Laboratories II, Nippon Shinyaku Co., Ltd.,
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KISE Masahiro
Discovery Research Laboratories II, Nippon Shinyaku Co., Ltd.,
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冨井 由文
Research Laboratories Nippon Shinyaku Co. Ltd.
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Matsuoka M
Department Of Environmental Toxicology Institute Of Industrial Ecological Sciences University Of Occ
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Segawa J
Research Laboratories Nippon Shinyaku Co. Ltd.
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Ozaki Masakuni
Discovery Research Laboratories Ii Nippon Shinyaku Co. Ltd.
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Honmura Takuya
Discovery Research Laboratories Ii Nippon Shinyaku Co. Ltd.
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