Studies on the Synthesis of Cholecystokinin A Receptor Antagonists. II. Synthesis and Cholecystokinin A Receptor Inhibitory Activities of Sulfur-Containing Amide-Carboxylic Acid Derivatives

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Other Title
  • コレシストキニンA受容体拮抗剤の合成研究(第2報)含硫アミドカルボン酸誘導体の合成とコレシストキニンA受容体阻害作用
  • コレシストキニン A ジュヨウタイ キッコウザイ ノ ゴウセイ ケンキュウ ダ

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Abstract

A number of sulfur-containing amide-carboxylic acid derivatives were synthesized and tested for cholecystokinin A (CCK-A) receptor inhibitory activity in order to study structure-activity relationships. Significant CCK-A receptor inhibitory activities were found in only two series, that is, sulfoxide-carboxylic acid derivatives (9) and sulfone-carboxylic acid derivatives (10). As the most preferred compound, 5-(3, 4-dichlorophenylsulfonyl)-4-(N, N-dipentylcarbamoyl)pentanoic acid (10n) was selected.

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 116 (5), 396-410, 1996

    The Pharmaceutical Society of Japan

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