Structure-Activity Study of Diuretic Azanaphthalene Derivatives

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概要

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• Regression analysis by the Free-Wilson technique was applied to estimate the contribution of substituents on azanaphthalene skeletons to diuretic activity of pyrimido [4,5-d] pyridazine and pyrido [3,4-d] pyridazine derivatives. In the former group, one of the most preferable compounds was 2-phenyl-5,8-dimorpholinopyrimido [4,5-d] pyridazine and that in the latter group proved to be 1,4-dimorpholine-7-phenylpyrido [3,4-d] pyridazine. Subsequently, electron density distributions on a variety of azanaphthalene skeletons were calculated by extended Huckel Theory calculation. Linear multiple regression analysis to find a correlation between diuretic activity and electron density at some positions of azanaphthalene skeletons suggested that the diuretic activity might be influenced largely by electronic structures at the ring junction.

• 社団法人日本薬学会の論文
• 1976-09-25

著者

• 西川 浩平

  日本製薬株式会社研究本部

• 西川 浩平

  Pharamaceutical Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industries

• 西川 浩平

  Central Research Division, Takeda Chemical Industries, Ltd.,

• 水田 栄治

  Central Research Division, Takeda Chemical Industries, Ltd.

• 大村 晴

  Central Research Division, Takeda Chemical Industries, Ltd.

• 岡 良和

  Central Research Division, Takeda Chemical Industries, Ltd.

• 大村 晴

  Medicinal Research Laboratories, Central Research Division, Takeda Chemical Industries, Ltd.

• 大村 晴

  Medicinal Research Laboratories Central Research Division Takeda Chemical Industries Ltd.

• 岡 良和

  Chemistry Laboratories Central Research Division Takeda Chemical Industries Ltd.

• 水田 栄治

  武田薬品工業

• 水田 栄治

  Central Research Division Takeda Chemical Industries Ltd.

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