Synthesis and Platelet-Activating Factor (PAF)-Antagonistic Activities of Trisubstituted Piperazine Derivatives
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概要
- 論文の詳細を見る
2- or 3-Substituted 1-(2,3-dimethoxy-6,7-dihydro-5H-benzocyclobepten-8- ylcarbonyl)-4-(3,4,5-trimethoxybenzoyl)- and 4-(3,4,5- trimethoxybenzyl)piperazines (2a - s, 3a, b) were prepared and evaluated for antagonistic activities against platelet-activating factor (PAF)-induced platelet aggregation and blood pressure reduction. The 2-methoxymethyl derivative (2f) showed the most potent activities in this series. The enantiomers (R)-(+)-2f and (S)-(-)-2f were synthesized from carbobenzoxy-O- benzyl-L- and D-serine in several steps. In the binding experiment. (S)-(-)- 2f showed thirty times greater affinity than the R isomer for the PAF receptor.
- 社団法人日本薬学会の論文
- 1994-03-15
著者
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馬渕 宏
Pharamaceutical Research Laboratories Ii Pharmaceutical Research Division Takeda Chemcial Industries
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西川 浩平
日本製薬株式会社研究本部
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西川 浩平
Pharamaceutical Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industries
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福士 英人
Pharmaceutical Research Laboratories I, Pharmaceutical Research Division, Takeda Chemical Industries
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馬渕 宏
Pharmaceutical Research Laboratories II, Pharmaceutical Research Division, Takeda Chemical Industrie
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寺下 善一
Research on Research, Pharmaceutical Research Division, Takeda Chemical Industries, Ltd.,
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西川 浩平
Pharmaceutical Research Laboratories I, Pharmaceutical Research Division, Takeda Chemical Industries
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杉原 弘貞
Pharmaceutical Research Laboratories I, Pharmaceutical Research Division, Takeda Chemical Industries
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寺下 善一
Research On Research Pharmaceutical Research Division Takeda Chemical Industries Ltd.
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福士 英人
Pharamaceutical Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industries
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杉原 弘貞
Pharamaceutical Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industries
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