Synthesis and Evaluation of Novel Thiazolidine Derivatives as Thromboxane A_2 Receptor Antagonists

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概要

• 論文の詳細を見る

• A series of 3-benzoyl or 3-phenylsulfonyl-2-substituted thiazolidine derivatives were synthesized, and evaluated for their thromboxane A_2 (TXA_2) receptor-antagonizing effect on (15S)-15-hydroxy-11α, 9α-(epoxymethano)prosta-5(Z), 13(E)-dienoic acid (U-46619)-induced aggregation of rabbit platelet-rich plasma (PRP). A simple 2-aryl-thiazolidine derivative, 3-benzoyl-2-(4-hydroxy-3-methoxyphenyl)thiazolidine (5a), showed mild TXA_2 receptor antagonist activity. Modification of 5a led to 2-chloro-4-[3-(4-chlorophenylsulfonyl)thiazolidin-2-ylmethyl]phenoxy-acetic acid (29d), which showed 10 times more potent TXA_2 receptor antagonist activity than 5a.

• 社団法人日本薬学会の論文
• 1994-03-15

著者

• 今西 武

  Faculty Of Pharmaceutical Sciences Osaka University

• 佐藤 正和

  成均館大学校

• 佐藤 正和

  大正製薬

• 川島 豊

  Research Center, Taisho Pharmaceutical Co., Ltd.

• 佐藤 正和

  Research Center, Taisho Pharmaceutical Co., Ltd.

• 岩田 宙造

  Faculty of Pharmaceutical Sciences, Osaka University

• 千葉 義行

  Central Research Laboratory, Nihon Suisan Kaisha, Ltd.,

• 佐竹 幹雄

  Central Research Laboratory, Nihon Suisan Kaisha, Ltd.,

• 五藤 准

  Research Center Taisho Pharm. Co., Ltd.,

• 山根 裕子

  Research Center Taisho Pharm. Co., Ltd.,

• 神野 修次

  Central Research Laboratory Nippon Suisan Kaisha, Ltd.,

• 川島 豊

  Research Center Taisho Pharmaceutical Co. Ltd.

• 川島 豊

  大正製薬・総合研

• 神野 修次

  Central Research Laboratory Nippon Suisan Kaisha Ltd.

• 岩田 宙造

  阪大院薬

• 佐藤 正基

  School Of Pharmaceutical Sciences University Of Shizuoka(present Address):marusa Corporation

• 岩田 宙造

  Faculty Of Pharmaceutical Sciences Osaka University

• Satoh M

  Showa Pharmaceutical Univ. Tokyo Jpn

• Sato M

  Otsuka Pharmaceutical Co. Ltd. Tokushima Jpn

• 佐竹 幹雄

  日本水産

• 五藤 准

  Research Center Taisho Pharm. Co. Ltd.

• 佐藤 真友美

  Univ. Shizuoka Shizuoka Jpn

• 佐藤 正和

  Research Center Taisho Pharmaceutical Co. Ltd.

• 千葉 義行

  Central Research Laboratory Nihon Suisan Kaisha Ltd.

• 山根 裕子

  Research Center Taisho Pharm. Co. Ltd.

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