Synthesis and Platelet Aggregation Inhibitory Activity of Diphenylazole Derivatives. I. Thiazole and Imidazole Derivatives
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概要
- 論文の詳細を見る
Diphenylimidazole and diphenylthiazole derivatives were synthesized and tested as inhibitors of platelet aggregation in in vitro experiments with the rabbit. Diphenylthiazole derivatives (10) were more potent than diphenylimidazole derivatives (4) in inhibiting arachidonic acid-induced platelet aggregation of rabbit platelet-rich plasma. Two diphenylimidazole and eight diphenylthiazole derivatives were evaluated for ex vivo arachidonic acid and collagen-induced platelet aggregation inhibitory activity using guinea pigs. In these compounds, 4,5-bis(4-methoxyphenyl)-2-(1,5-dimethyl-2-pyrrolyl)thiazole (10n) showed strong activity in vitro and ex vivo. The ex vivo activity of 10n was 200 times stronger than that of aspirin. The mechanism of the activity of 10n was the inhibition of cyclo-oxygenase.
- 公益社団法人日本薬学会の論文
- 1991-03-25
著者
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横田 耕一
鐘紡
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塚本 悟郎
Pharmaceuticals Research Center, Kanebo Ltd.
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吉野 公一郎
Pharmaceuticals Research Center Kanebo Ltd.
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塚本 悟郎
New Drug Research Laboratories Kanebo Ltd.
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横田 耕一
Pharmaceuticals Research Center Kanebo Ltd.
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世古 典彦
Pharmaceuticals Research Center, Kanebo Ltd.,
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世古 典彦
Pharmaceuticals Research Center Kanebo Ltd.
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塚本 悟郎
Pharmaceutical Research Laboratory, Tanabe Seiyaku Co., Ltd.
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