Antivertigo Agents. II. Structure-Activity Relationships of 6-Substituted 5,6,7,8-Tetrahydro-1,6-naphthyridines
スポンサーリンク
概要
- 論文の詳細を見る
A number of 6-substituted 5,6,7,8-tetrahydro-1,6-naphthyridines designed as cyclic homologues of betahistine, 2-(2-methylaminoethyl) pyridine, were synthesized by the reduction of the corresponding 1,6-naphthyridinium salts. The antivertigo activity of these derivatives was evaluated in terms of their ability to inhibit spontaneous nystagmus in cats. The relationships between the molecular structures of the test compounds and their antivertigo activities were investigated by a regression analysis based on the lipophilicity (π) of the substituents at the 6-position and by a conformational analysis of the compounds of interest using the modified neglect of diatomic overlap molecular orbital method. Among these compounds, the 6-allyl-and 6-cyclopropylmethyl derivatives exhibited extremely potent activity with greatly reduced hypotensive action.
- 社団法人日本薬学会の論文
- 1984-03-25
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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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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古後 義也
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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古後 義也
Research Laboratories Of Pharmaceutical Division Nippon Kayaku Co.
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坂本 尚夫
Pharmaceutical Institute Tohoku University
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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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