Studies on the Synthesis of Cholecystokinin A Receptor Antagonists. I. Synthesis and Cholecystokinin A Receptor Inhibitory Activities of Malonamide Derivatives

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  • コレシストキニンA受容体拮抗剤の合成研究(第1報)Malonamide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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Description

2-Substituted malonamide derivatives were synthesized and tested for cholecystokinin A (CCK-A) receptor inhibitory activity. Significant CCK-A receptor inhibitory activities were found in only three compounds (4g-i) which have carboxyl group. In order to study structure-activity relationships, carboxyethyl group was selected for 2-substituent and a number of N-substituted malonamides were prepared. After these compounds were tested for CCK-A receptor inhibitory activity, 4-(3, 4-dichlorophenylcarbamoyl)-N, N-dipentylglutaramic acid (4h) was selected as the most preferred compound.

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 116 (1), 50-58, 1996

    The Pharmaceutical Society of Japan

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