Design and Synthesis of Piperazinylpyridine Derivatives as Novel 5-HT1A Agonists/5-HT3 Antagonists for the Treatment of Irritable Bowel Syndrome (IBS)
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- Asagarasu Akira
- Synthetic Research Department, ASKA Pharmaceutical Co., Ltd.
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- Matsui Teruaki
- Synthetic Research Department, ASKA Pharmaceutical Co., Ltd.
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- Hayashi Hiroyuki
- Synthetic Research Department, ASKA Pharmaceutical Co., Ltd.
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- Tamaoki Satoru
- Pharmacological Research Department, ASKA Pharmaceutical Co., Ltd.
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- Yamauchi Yukinao
- Pharmacological Research Department, ASKA Pharmaceutical Co., Ltd.
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- Sato Michitaka
- Synthetic Research Department, ASKA Pharmaceutical Co., Ltd.
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説明
We have prepared a series of piperazinylpyridine derivatives for the treatment of irritable bowel syndrome (IBS). These compounds, which were designed by pharmacophore analysis, bind to both serotonin subtype 1A (5-HT1A) and subtype 3 (5-HT3) receptors. The nitrogen atom of the isoquinoline, a methoxy group and piperazine were essential to the pharmacophore for binding to these receptors. We also synthesized furo- and thienopyridine derivatives according to structure–activity relationship analyses. Compound 17c (TZB-20810) had high affinities to these receptors and exhibited 5-HT1A agonistic activity and 5-HT3 antagonistic activity concurrently, and is a promising drug for further development in the treatment of IBS.
収録刊行物
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- ＣＨＥＭＩＣＡＬ ＆ ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ ＢＵＬＬＥＴＩＮ
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ＣＨＥＭＩＣＡＬ ＆ ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ ＢＵＬＬＥＴＩＮ 57 (1), 34-42, 2009
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679146260736
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- NII論文ID
- 110007021618
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 9749586
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可
