New β-Adrenoreceptor Stimulants. Studies on 3-Acylamino-4-hydroxy-α-(N-substituted aminomethyl) benzyl Alcohols

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概要

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• New β-adrenergic stimulants, 3-acylamino-4-hydroxy-α-(N-substituted aminomethyl)-benzyl alcohols (VIII) were prepared via 3-amino-4-benzyloxy-α-(N-substituted aminomethyl) benzyl alcohols (V) in several steps. These agents were catecholamine derivatives, in which m-phenolic OH was replaced by acylamino and substituted acylamino groups. Terbutaline analogues (XIXa, b, XX), in which one or both of two phenolic OH were replaced by formamido or methoxycarboxamido groups were synthesized, too. Compounds (VIIIa, c, 1-q) bearing formylamino group in the meta position showed potent β_2-stimulant activity in vitro. In these, N-phenylalkyl series were more potent β_2-stimulant than N-alkyl series. Several compounds, which bear two asymmetric centers, were separated into two racemates and the β_2-stimulant activity of them were different. From these compounds, 3-formamido-4-hydroxy-α-(N-(p-methoxy-α-methylphenethyl) aminomethyl)-benzyl alcohol ・1/2 fumarate (VIIIn-A) (BD-40-A) was selected as the best compound.

• 公益社団法人日本薬学会の論文
• 1977-06-25

著者

• 高橋 孝三

  山之内製薬中央研究所

• 村上 増雄

  Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.

• 高橋 孝三

  Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.

• 村瀬 清志

  Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.

• 間瀬 年康

  Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.

• 井田 昶

  Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.

• 村瀬 清志

  Gastrointestinal Research Laboratories Institute For Drug Discovery Research Yamanouchi Pharmaceutic

• Murase Kiyoshi

  Neuroscience/gastrointestinal Research Laboratories Institute For Drug Discovery Research Yamanouchi

• 井田 昶

  Central Research Laboratories Yamanouchi Pharmaceutical Co. Ltd.

• 間瀬 年康

  Central Research Laboratories Yamanouchi Pharmaceutical Co. Ltd.

• 高橋 孝三

  Central Research Laboratories Yamanouchi Pharmaceutical Co. Ltd.

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