2-(3-Pyridyl)thiazolidine-4-carboxamides. 1. Novel Orally Active Antagonists of Platelet-Activating Factor (PAF)

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概要

• 論文の詳細を見る

• In a search for novel platelet-activating factor (PAF) antagonists, we found that 1-(3-phenylpropyl)-4-[2-(3-pyridyl)thiazolidine-4-carboyl]piperazine (3%) showed in vitro and in vivo PAF-antagonistic activities. Introduction of functional groups at the benzylic methylene carbon of 3x afforded some compounds with more potent PAF-antagonistic activity than 3x. Among them 1-(3-methyl-3-phenylbutyl)-4-[2-(3-pyridyl)thiazolidine-4-carbonyl]-piperazine fumarate (3al, YM264) was found to be one of the most potent PAF antagonists.

• 1997-10-15

著者

• 斎藤 徹

  Faculty Of Pharmaceutical Sciences Kanazawa University

• SUZUKI Takeshi

  Institute for Solid State Physics, University of Tokyo

• Suzuki T

  Drug Discovery Research Laboratory Sanwa Kagaku Kenkyusho Co. Ltd.

• Hara Hideaki

  Research And Development Center Santen Pharmaceutical Co. Ltd.

• Suzuki T

  Laboratory Of Biopharmaceutics Faculty Of Pharmaceutical Sciences Chiba University

• Takeuchi M

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Takeuchi Makoto

  Chemistry Research Laboratories Astellas Pharmaceutical Inc.

• TAKEUCHI Makoto

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

• Takeuchi M

  Chemistry Research Laboratories Astellas Pharmaceutical Inc.

• Saito Takako

  Research And Development Laboratories Maruho Co. Ltd.

• YAMADA Tatsuhiko

  Pharmaceutical Laboratories, Kissei Pharmaceutical Co., Ltd.,

• MATSUHISA Akira

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

• Matsuhisa Akira

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Suzuki Toshikazu

  Discovery Research Laboratory Tanabe Seiyaku Co. Ltd.

• Yamada T

  Department Of Radiopharmacy Tohoku Pharmaceutical University

• TOMIOKA Kenichi

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

• YAMADA Toshimitsu

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

• SAITO Munetoshi

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co.

• NAGAOKA Hitoshi

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

• HARA Hiromu

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

• MASE Toshiyasu

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

• TAKAHASHI Takumi

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

• Tomioka K

  Graduate School Of Pharmaceutical Sciences Kyoto University

• Saito M

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co.

• Suzuki T

  Research Unit Of Pharmaceutics College Of Pharmacy Nihon University

• Yamada Takehisa

  Research And Development Division Hokuriku Seiyaku Co. Ltd.

• Takahashi T

  Department Of Pharmacology Graduate School Of Pharmaceutical Sciences Hokkaido University

• Hara H

  (present Address)corporate Planning Dept. Yamanouchi Pharmaceutical Co. Ltd.

• Mase T

  Yamanouchi Pharmaceutical Co. Ltd. Ibaraki Jpn

• Matsuhisa Akira

  Institute For Drug Discovery Research Astellas Pharma Inc.

• Suzuki Takeshi

  Institute For Molecular And Cellular Regulation Gunma University

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