Nonpeptide Arginine Vasopressin Antagonists for Both V_<1A> and V_2 Receptors : Synthesis and Pharmacological Properties of 2-Phenyl-4'-(2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-1-carbonyl)benzanilide Derivatives

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概要

• 論文の詳細を見る

• A series of compounds structurally related to 2-phenyl-4'-(2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-1-carbonyl)benzanilide was synthesized and demonstrated to have arginine vasopressin (AVP) antagonist activity for both V_<1A> and V_2 receptors. The introduction of a hydrophilic substituent group into the 5-position of the benzodiazepine ring resulted in an increase in oral availability. Especially, the (3-pyridyl)methyl (31b), the 2-(4-methyl-1,4-diazepan-1-yl)-2-oxoethyl (32i), and the 2-(4-methylpiperazin-1-yl)ethyl (33g) derivatives exhibited high antagonist activities and high oral availability. Details of the synthesis and pharmacological properties of this series are presented.

• 公益社団法人日本薬学会の論文
• 1998-10-15

著者

• TANAKA Akihiro

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

• Tanaka A

  Faculty Of Pharmaceutical Sciences Tokyo University Of Science

• Tanaka A

  Yamanouchi U.k. Ltd. Surrey Gbr

• 増田 明

  富山医科薬科大学麻酔科

• TANIGUCHI Nobuaki

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

• MATSUHISA Akira

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

• YATSU Takeyuki

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

• Yatsu Takeyuki

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Matsuhisa Akira

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Matsuhisa Akira

  Gastrointestinal Research Laboratories Institute For Drug Discovery Research Yamanouchi Pharmaceutic

• Taniguchi Nobuaki

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Tanaka Akihiro

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• KOSHIO Hiroyuki

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co. Ltd.

• Koshio Hiroyuki

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• SAKAMOTO Kenichiro

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,

• Yatsu Takeyuki

  Astellas Pharma Inc. Ibaraki Jpn

• Tahara Atsuo

  Drug Discovery Research Astellas Pharma Inc.

• Sakamoto K

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Matsuhisa Akira

  Institute For Drug Discovery Research Astellas Pharma Inc.

• Koshio Hiroyuki

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,

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