Antivertigo Agents. I. Structure-Activity Relationships of 2-(2-Aminoethyl) pyridines
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概要
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A series of 2-(2-aminoethyl) pyridines derived by the modification of the amine moiety in betahistine, 2-(2-methylaminoethyl) pyridine, was synthesized and evaluated for antivertigo action in terms of inhibitory activity against spontaneous nystagmus in cats. The structure-activity relationships between the amine moieties and antivertigo activities were investigated. The effects of substituents on the phenyl ring of the 4-phenylpiperazine moiety were investigated by means of quantitative regression analysis using various physicochemical parameters. The following equation gave the best correlation. log 1/ID_<30>=-0.417 (±0.322) π+0.166 (±0.048) MR-1.473 (±0.237) (n=15,s=0.239,r=0.910,F^2_<12>=28.887). In this series of compounds, 1-(2-methoxyphenyl)-4-[2-(2-pyridyl) ethyl] piperazine, 1-(2-methoxyphenyl)-4-[2-[2-(6-methyl) pyridyl] ethyl]-piperazine, and 1-(2-methoxyphenyl)-4-[2-[2-(5-ethyl) pyridyl] ethyl] piperazine were found to show more potent activity than betahistine. Thus, the 4-(2-methoxyphenyl) piperazine group was found to be the most effective amine moiety for activity against spontaneous nystagmus.
- 社団法人日本薬学会の論文
- 1984-02-25
著者
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宮崎 浩
日本化薬(株)経営企画室
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坂本 尚夫
Pharmaceutical Institute, Tohoku University
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山中 宏
Pharmaceutical Institute, Tohoku University
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塩沢 明
日本化薬
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塩沢 明
Research Laboratories of Pharmaceutical Division, Nippon Kayaku Co.
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市川 裕一郎
Research Laboratories of Pharmaceutical Division, Nippon Kayaku Co.
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小室 主税
Research Laboratories of Pharmaceutical Division, Nippon Kayaku Co.
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石川 道雄
Research Laboratories of Pharmaceutical Division, Nippon Kayaku Co.
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蔵重 修二
Research Laboratories of Pharmaceutical Division, Nippon Kayaku Co.
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市川 裕一郎
Faculty of Pharmaceutical Sciences, Chiba University
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宮崎 浩
Research Laboratories of Pharmaceuticals Group, Nippon Kayaku Co., Ltd.,
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井津 源市
Research Laboratories of Pharmaceutical Division, Nippon Kayaku Co.
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石川 道雄
Research Laboratories Of Pharmaceutical Division Nippon Kayaku Co.
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坂本 尚夫
Pharmaceutical Institute Tohoku University
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小室 主税
Research Laboratories Of Pharmaceutical Division Nippon Kayaku Co.
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井津 源市
Research Laboratories Of Pharmaceutical Division Nippon Kayaku Co.
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市川 裕一郎
Faculty Of Pharmaceutical Sciences Chiba University
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蔵重 修二
Research Laboratories of Pharmaceuticals Group, Nippon Kayaku CO., Ltd.,
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