Synthesis and Platelet-Activating Factor (PAF)-Antagonistic Activities of 1,4-Disubstituted Piperazine Derivatives

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概要

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• During the screening of novel platelet-activating factor (PAF) antagonists, we found that 1-(6-methoxy-3,4-dihydro-2-naphthoyl)-4-(3,4,5-trimethoxybenzyl)piperazine and its 4-(3,4,5-trimethoxybenzoyl)piperazine derivatives (1b, 2b) exerted in vitro and in vivo PAF-antagonistic activities. Modifications of the 1-acyl group, the substituent at the 4-position and the piperazine ring of 1a and 2b were examined and from this series 1-(2,3-dimethoxy-6,7-dihydro-5H-benzocyclohepten-8-ylcarbonyl)-4-(3,4,5-trimethoxybenzoyl)piperazine (2g) was found to be one of the most potent PAF antagonists.

• 社団法人日本薬学会の論文
• 1994-03-15

著者

• 馬渕 宏

  Pharamaceutical Research Laboratories Ii Pharmaceutical Research Division Takeda Chemcial Industries

• 西川 浩平

  日本製薬株式会社研究本部

• 西川 浩平

  Pharamaceutical Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industries

• 伊藤 克己

  Pharmaceutical Research Laboratories Iii Pharmaceutical Research Division Takeda Chemical Industries

• 寺下 善一

  Research on Research, Pharmaceutical Research Division, Takeda Chemical Industries, Ltd.,

• 福士 英人

  Pharamaceutical Research Laboratories, I, Pharmaceutical Research Division, Takeda Chemical Industri

• 伊藤 克己

  Pharamaceutical Research Laboratories, III, Pharmaceutical Research Division, Takeda Chemical Indust

• 杉原 弘貞

  Pharamaceutical Research Laboratories, I, Pharmaceutical Research Division, Takeda Chemical Industri

• 寺下 善一

  Research On Research Pharmaceutical Research Division Takeda Chemical Industries Ltd.

• 福士 英人

  Pharamaceutical Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industries

• 伊藤 克巳

  武田薬品工業

• 伊藤 克已

  Central Research Division Takeda Chemical Industries Ltd.

• 杉原 弘貞

  Pharamaceutical Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industries

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