2-(3-Pyridyl)thiazolidine-4-carboxamide Derivatives. II. Structure-Activity Relationships and Active Configuration of 2-(3-Pyridyl)thiazolidine-4-carboxamides as Platelet-Activating Factor Receptor Antagonists

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概要

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• Conversion of the 2-(3-pyridyl)thiazolidine part of 1-(3-phenylpropyl)-4-[2-(3-pyridyl)thiazolidine-4-carbonyl]piperazine (YM461), which is a potent platelet-activating factor (PAF) antagonist, to other rings was performed, and PAF antagonistic activities evaluated. The 2-(3-pyridyl)thiazolidine skeleton, which exists as a mixture of cis and trans diastereomers, played an important role in the potency of PAF antagonism. In this study, new effect skeletons were not uncovered, however, 2-(4-pyridyl)thiazolidine-4-carboxamides (1n and 1z) showed potent PAF antagonistic activities equal to the 3-pyridyl derivatives. From the results obtained for 1a, 1a(S), 1g and 1i, a cis-(2R, 4R)-2-(3-pyridyl)thiazolidine-4-carboxamide was assumed to be the active configuration for PAF antagonism.

• 1998-09-15

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.

• Kondo Y

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• 鈴木 徳治

  千葉大 薬

• 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.

• Kondo Yutaka

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Saito T

  Research And Development Headquarters Hokurikit Seiyaku Co. Ltd.

• Saito Takako

  Research And Development Laboratories Maruho Co. Ltd.

• YAMADA Tatsuhiko

  Pharmaceutical Laboratories, Kissei Pharmaceutical Co., Ltd.,

• Suzuki Toshikazu

  Discovery Research Laboratory Tanabe Seiyaku Co. Ltd.

• Yamada T

  Department Of Radiopharmacy Tohoku Pharmaceutical University

• Hamada Mamoru

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• 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.

• Sugihara T

  Faculty Of Pharmaceutical Sciences Tokushima Bunri University

• Takahashi T

  Department Of Pharmacology Graduate School Of Pharmaceutical Sciences Hokkaido University

• Saito T

  Research And Development Laboratories Maruho Co. Ltd.

• Hara H

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

• Mase T

  Yamanouchi Pharmaceutical Co. Ltd. Ibaraki Jpn

• Suzuki Takeshi

  Institute For Molecular And Cellular Regulation Gunma University

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