Structure-Activity Study of Anti-inflammatory Trioxoper-hydropyrimidine Derivatives
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概要
- 論文の詳細を見る
Regression analyses using the Free-Wilson technique were applied to the anti-inflam-matory effect and the acute toxicity of 57 1,3,5-trisubstituted 2,4,6-trioxoperhydropyrimidine derivatives. Models for the orientation of substituents on the "receptor site" are presented. A significant correlation was obtained by assuming that one of the N-substituents with a high hydrophobicity always locates at a particular binding site. Further analysis of the contributions of substituents at the 5-position using the free energy related hydrophobic parameter, π revealed that acute toxicity increases with an increase in the hydrophobicity of the 5-substituents. 1-Cyclohexyl-5-butyl or -allyl derivatives seemed to be the most suitable anti-inflammatory agents in terms of their high activity and low toxicity.
- 公益社団法人日本薬学会の論文
- 1975-01-25
著者
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藤田 稔夫
Department of Agricultural Chemistry, Kyoto University
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藤田 稔夫
Emil Project Fujitsu Kansai Systems Laboratory
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藤田 稔夫
Department Of Agricultural Chemistry Kyoto University
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西川 正夫
Chemical Research Laboratories, Central Research Division, Takeda Chemical Industries, Ltd.
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西川 正夫
Central Research Division, Takeda Chemical Industries, Ltd.
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西川 正夫
Central Research Division Takeda Chemical Industries Ltd.
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水田 栄治
武田薬品工業
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