ドーパミンβ-水酸化酵素阻害活性を持つ6-アルキルアミノピリダジン-3-カルボン酸誘導体の合成

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書誌事項

タイトル別名
  • Synthesis of 6-Alkylaminopyridazine-3-carboxylic Acid Derivatives as Dopamine β-Hydroxylase Inhibitors
  • ドーパミン ベータ スイサンカ コウソ ソガイ カッセイ オ モツ 6 アルキ
  • Synthesis of 6-Alkylaminopyridazine-3-carboxylic Acid Derivatives as Dopamine β-Hydroxylase Inhibitors

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抄録

A series of 6-alkylaminopyridazine-3-carboxylic acid derivatives was tested for dopamine β-hydroxylase inhibitory activity in vitro according to the method of Kruse et al. Methyl 6-alkylaminopyridazine-3-carboxylates (4) were synthesized through the reaction of methyl 6-chloropyridazine-3-carboxylate (1) with ammonia followed by the condensation with primary amines, and by the methanolysis of the resulting 6-alkylaminopyridazine-3-carboxa-mides (3) in methanol in the presence of boron trifluoride etherate. Among tested compounds, 6-benzylaminopyridazine-3-carboxylic acid was found to have the most potent inhibitory activity, which was in the same level of the activity of fusaric acid.

収録刊行物

  • 薬学雑誌

    薬学雑誌 112 (10), 768-772, 1992

    公益社団法人 日本薬学会

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