Synthesis and Evaluation of Novel Thiazolidine Derivatives as Thromboxane A2 Receptor Antagonists

Masakazu SATO; Yutaka KAWASHIMA; Jun GOTO; Yuuko YAMANE; Yoshiyuki CHIBA; Shuji JINNO; Mikio SATAKE; Takeshi IMANISHI; Chuzo IWATA

doi:10.1248/cpb.42.521

Synthesis and Evaluation of Novel Thiazolidine Derivatives as Thromboxane A₂ Receptor Antagonists

佐藤正和, 川島豊, 五藤准, 山根裕子, 千葉義行, 神野修次, 佐竹幹雄, 今西武, 岩田宙造

著者情報

キーワード: thromboxane A₂, TXA₂, receptor, antagonist, thiazolidine, structure-activity relationship

ジャーナルフリー

1994 年 42 巻 3 号 p. 521-529

DOI https://doi.org/10.1248/cpb.42.521

詳細

抄録

A series of 3-benzoyl or 3-phenylsulfonyl-2-substituted thiazolidine derivatives were synthesized, and evaluated for their thromboxane A₂ (TXA₂) 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 TXA₂ 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 TXA₂ receptor antagonist activity than 5a.

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