New Intracellular Calcium Antagonists. I. Synthesis and Pharmacological Evaluation of 2, 3, 4, 5-Tetrahydro-1, 5-benzothiazepine Analogs

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  • 新しい細胞内カルシウム抑制薬の研究(第1報)2,3,4,5-Tetrahydro-1,5-benzothiazepine誘導体の合成とその薬理作用
  • アタラシイ サイボウナイ カルシウム ヨクセイヤク ノ ケンキュウ ダイ 1ポ

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Description

A series of 2, 3, 4, 5-tetrahydro-1, 5-benzothiazepine and related compounds were prepared, and the intracellular Ca2+ inhibitory effects were examined using methoxamine-or caffeine-induced contraction of isolated rabbit arteries. Structure-activity relationship studies of these compounds are discussed and the results suggest that novel 5-[3-[2-(3, 4-dimethoxyphenyl) ethyl] aminopropionyl]-2, 3, 4, 5-tetrahydro-1, 5-benzothiazepine fumarate (20d) showed the most potent inhibitory action on the intracellular Ca2+ release.

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 116 (2), 106-124, 1996

    The Pharmaceutical Society of Japan

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