Structure-Activity Relationships of Non-peptide Vasopressin V_<1a> Antagonists : 1-(1-Multi-substituted Benzoyl 4-Piperidyl)-3,4-dihydro-2(1H)-quinolinones

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概要

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• During our systematic studies on the arginine vasopressin receptor V_<1a>-antagonistic activity of 1-(1-benzoyl substituted 4-piperidyl)-3,4-dihydro-2(1H)-quinolinones, we found a general substituent effect on the benzene ring. Hydrogen-bonding ability at the ortho position was especially important for enhancement of the affinity of multi-substituted analogs. Details of the syntheses and structuer-activity relationships for this series are presented.

• 公益社団法人日本薬学会の論文
• 1996-04-15

著者

• Yamamura Y

  First Institute Of New Drug Research Otsuka Pharmaceutical Co. Ltd.

• TOMINAGA Mineko

  Department of Biophysics, Universidade Federal de Sao Paulo

• Kondo Kazumi

  Second Institute Of New Drug Research Otsuka Pharmaceutical Co. Ltd.

• Tominaga M

  Department Of Biophysics Universidade Federal De Sao Paulo

• Yabuuchi Y

  First Institute Of New Drug Research Otsuka Pharmaceutical Co. Ltd.

• Ogawa H

  Second Institute Of New Drug Research Otsuka Pharmaceutical Co. Ltd.

• OGAWA Hidenori

  Second Institute of New Drug Research, Otsuka Pharmaceutical Co., Ltd.,

• KNAKAYA Kenji

  Second Institute of New Drug Research, Otsuka Pharmaceutical Co., Ltd.,

• TOMINAGA Michiaki

  Second Institute of New Drug Research, Otsuka Pharmaceutical Co., Ltd.,

• YABUUCHI Youichi

  Second Institute of New Drug Research, Otsuka Pharmaceutical Co., Ltd.,

• Knakaya Kenji

  Second Institute Of New Drug Research Otsuka Pharmaceutical Co. Ltd.

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