Preparation of Highly Potent and Selective Non-Peptide Antagonists of the Arginine Vasopressin V_<1A> Receptor by Introduction of a 2-Ethyl-1H-1-imidazolyl Group

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概要

• 論文の詳細を見る

• To find a new series of arginine vasopressin (AVP) V_<1A> receptor antagonists, the influence of the 2-phenyl group of 2-phenyl-4'-[(2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl]benzanilide (7) was investigated. Replacement of the 2-phenyl group by a 2-ethyl-1H-imidazol-1-yl group was effective in yielding a V_<1A>-selective compound. Moreover, this imidazolyl group was introduced in the same position in YM-35471 (6), and further studies of these compounds were performed. Consequently, we found that the (Z)-4'-({4,4-difluoro-5-[(N-cyclo-propylcarbamoyl)methylene]-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl}carbonyl)-2-(2-ethyl-1H-1-imidazol-1-yl)benzanilide (9f) exhibited highly potent affinity and selectivity, and was the most potent antagonist for the V_<1A> receptor among our compounds. The synthesis and pharmacological evaluation of these compounds are described in this paper

• 公益社団法人日本薬学会の論文
• 2005-07-01

著者

• TANAKA Akihiro

  Corporate Communications Department, Yamanouchi Pharmaceutical Co., Ltd.

• Tsukada Junko

  Clinical Development Department 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

• Kawano Noriyuki

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• SHIMADA Yoshiaki

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

• AKANE Hiroaki

  Clinical Development Department, Yamanouchi Pharmaceutical Co., Ltd.

• TANIGUCHI Nobuaki

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

• MATSUHISA Akira

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

• KIKUCHI Kazumi

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

• YATSU Takeyuki

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

• TAHARA Atsuo

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

• TOMURA Yuichi

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

• KUSAYAMA Toshiyuki

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

• WADA Kohichi

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

• TSUNODA Takashi

  Chemical Technology Laboratory, Yamanouchi Pharmaceutical Co., Ltd.

• Wada Kohichi

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Akane Hiroaki

  Clinical Development Department Yamanouchi Pharmaceutical Co. Ltd.

• Kikuchi Kazumi

  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.

• Kusayama Toshiyuki

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Shimada Yoshiaki

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Yatsu Takeyuki

  Astellas Pharma Inc. Ibaraki Jpn

• Tanaka Akihiro

  Corporate Communications Department Yamanouchi Pharmaceutical Co. Ltd.

• Tomura Yuichi

  Drug Discovery Research, Astellas Pharma Inc.

• Tsunoda Takashi

  Chemical Technology Laboratory Yamanouchi Pharmaceutical Co. Ltd.

• Tahara Atsuo

  Drug Discovery Research Astellas Pharma Inc.

• Tomura Yuichi

  Drug Discovery Research Astellas Pharma Inc.

• Matsuhisa Akira

  Institute For Drug Discovery Research Astellas Pharma Inc.

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