Studies on biologically Active Halogenated Compounds. IV. Synthesis and Antibacterial Activity of Fluorinated Quinoline Derivatives
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概要
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Polyfluorinated derivatives of 1-alkyl-1,4-dihydro-7-methyl-4-oxoquinoline-3-carboxylic acids were synthesized and examined for antibacterial activites in vitro. Among the N-substituents, the strength of antibacterial activity of the derivatives was in the order : CH_2CH_2F>CH_2CH_3>CH_2CF_3>CHF_2. Introduction of two fluorine atoms at the 6 and 8 positions of the skeleton (21a, b) led to high activity, but substitution of the 7-methyl group (20,21,25) with a fluoromethyl group (40,41,48) led in general to reduced activity. Thus, 6,8-difluoro-1,4-dihydro-1-(2-fluoroethyl)-7-methyl-4-oxoquinoline-3-carboxylic acid (21b) showed the highest activity, almost equal to that of oxolinic acid.
- 公益社団法人日本薬学会の論文
- 1982-10-25
著者
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谷 醇一
Research Laboratory of Applied Biochemistry, Tanabe Seiyaku Co., Ltd.
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虫鹿 好孝
Research Laboratory Of Applied Biochemistry Tanabe Seiyaku Co. Ltd
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山口 東太郎
Microbiological Research Laboratory Tanabe Seiyaku Co. Ltd
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