Design and Syntheses of a Series of Novel Serotonin_3 Antagonists
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概要
- 論文の詳細を見る
From a structural comparison study between serotonin and serotonin_3 (5-HT_3) antagonists using a two-dimensional grid template composed of regular hexagons, we deduced structural modification patterns from agonists to antagonists, and designed new 5-HT_3 antagonist prototypes. Among them, 2-(4-methyl-1-piperazinyl)-1-butylbenzimidazole (6) was identified as a lead compound which has potent 5-HT_3 antagonistic activity comparable to that of granisetron. Using a quantitative structure-activity relationships method, we optimized the structure of 6 and selected 6-amino-5-chloro-1-isopropyl-2-(4-methyl-1-piperazinyl)benzimidazole dimaleate (69,KB-6933), one of the most potent and long-acting 5-HT_3 antagonists, as a candidate drug.
- 公益社団法人日本薬学会の論文
- 1993-10-15
著者
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大高 博
New Drug Research Laboratories Kanebo Ltd.
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中島 史雄
New Drug Research Laboratories Kanebo Ltd.
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鈴木 健司
New Drug Research Laboratories Kanebo Ltd.
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堀 学
New Drug Research Laboratories, Kanebo Ltd.,
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山本 武志
New Drug Research Laboratories, Kanebo Ltd.,
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尾崎 昭夫
New Drug Research Laboratories, Kanebo Ltd.,
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堀 学
New Drug Research Laboratories Kanebo Ltd.
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尾崎 昭夫
New Drug Research Laboratories Kanebo Ltd.
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