Synthetic Chemotherapeutic Agents. III. Synthesis of 3-Substituted Thiazolo [5,4-f] quinoline Derivatives. (1)
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概要
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For the search of the more active antimicrobial compounds than the 2,6-disubstituted derivatives, 3,6-disubstituted 2,3,6,9-tetrahydro-2,9-dioxothiazolo [5,4-f] quinoline-8-carboxylic acid (1,3,7,8,11,20,21,and 22) were synthesized from the 2-oxo-6-substituted thiazolo [5,4-f] quinoline derivatives (2,17,or 18). Thermal rearrangement of the 2-methylthio derivative (23) gave the 2-thioxo-3-methyl derivative (24), which was converted into the 2-oxo-3-methyl derivative (26) by reaction with mercuric acetate. The 2-ethoxy derivative (27) was also thermally rearranged to give the 2-oxo-3-ethyl derivative (8b). The 3,6-disubstituted compounds obtained in this work showed the stronger activities against gram-negative and gram-positive bacteria in vitro than nalidixic acid and the 2,6-disubstituted derivatives prepared in the previous work. 6-Ethyl-2,3,6,9-tetrahydro-3-methyl-9-oxothiazolo [5,4-f] quinoline-8-carboxylic acid (8a) exhibited the strongest activities among these compounds against many gram-negative bacteria including E. coli resistant to nalidixic acid and Ps. aeruginosa, and against some gram-positive bacteria.
- 公益社団法人日本薬学会の論文
- 1976-01-25
著者
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鈴木 範夫
Research Institute, Daiichi Seiyaku Co., Ltd.
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鈴木 範夫
Research Institute Daiichi Seiyaku Co. Ltd.
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門矢 静夫
Research Institute Daiichi Seiyaku Co. Ltd.
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堂森 廉三
Research Institute Daiichi Seiyaku Co. Ltd.
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高村 功
Research Institute, Daiichi Seiyaku Co., Ltd.
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高村 功
Research Institute Daiichi Seiyaku Co. Ltd.
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