1,5-Benzoxathiepin Derivatives. II. Synthesis and Serotonin S_2-Receptor-BIocking Activity of Aminoalkyl-Substituted 3,4-Dihydro-2H-1,5-benzoxathiepin-3-ols and Related Compounds(Medicinal Chemistry,Chemical)

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概要

• 論文の詳細を見る

• Novel 1,5-benzoxathiepin derivatives, 3,4-dihydro-2H-1,5-benzoxathiepin-3-ols with an aminoalkyl group at the 2-, 3- or 4-position, were synthesized and evaluated for scrotonin S_2-receptor-blocking activity and adrenergic α_1-receptor-blocking activity. Methyl 4-aminoalkyl-3-hydroxy-3,4-dihydro-2H-1,5-benzoxathiepin-4-carboxylates showed significant S_2-receptor-blocking activities. Structure-activity relationships (including the results of a conf ormational study and skeletal modifications) were examined. In the series of 1,5-benzoxathiepin, 1-benzoxepin and 1-benzothiepin derivatives, methyl cis-3-hydroxy-7-methoxy-4-[3-(4-phenyl-1-piperazinyl)propyl]-3,4-dihydro-2H1,5-benzoxathiepin-4-carboxylate hydrochloride (CV-5197) showed the most potent and the most selective S_2-receptor-blocking activity in the binding profile, and was chosen as a candidate for further pharmacological evaluation.

• 社団法人日本薬学会の論文
• 1987-05-25

著者

• 馬渕 宏

  Pharamaceutical Research Laboratories Ii Pharmaceutical Research Division Takeda Chemcial Industries

• 川松 豊

  Central Research Division, Takeda Chemical Industries, Ltd.,

• 杉原 弘貞

  Central Research Division, Takeda Chemical Industries, Ltd.,

• 馬渕 宏

  Central Research Division, Takeda Chemical Industries, Ltd.

• 平田 稔

  Central Research Division, Takeda Chemical Industries, Ltd.

• 今本 哲治

  Central Research Division, Takeda Chemical Industries, Ltd.

• 川松 豊

  干寿製薬株式会社経営戦略室

• 平田 稔

  Central Research Division Takeda Chemical Industries Ltd.

• 杉原 弘貞

  Central Research Division Takeda Chemical Industries. Ltd.

• 今本 哲治

  Central Research Division Takeda Chemical Industries Ltd.

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