Design and Synthesis of Piperazinylpyridine Derivatives as Novel 5-HT_<1A> Agonists/5-HT_3 Antagonists for the Treatment of Irritable Bowel Syndrome (IBS)

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概要

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• 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-HT_<1A>) and subtype 3 (5-HT_3) 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-HT_<1A> agonistic activity and 5-HT_3 antagonistic activity concurrently, and is a promising drug for further development in the treatment of IBS.

• 公益社団法人日本薬学会の論文
• 2009-01-01

著者

• TAMAOKI Satoru

  Pharmacological Research Department

• Sato Michitaka

  Synthetic Research Department Aska Pharmaceutical Co. Ltd.

• Matsui Teruaki

  Synthetic Research Department Aska Pharmaceutical Co. Ltd.

• Tamaoki Satoru

  Pharmacological Research Department Aska Pharmaceutical Co. Ltd.

• ASAGARASU Akira

  Synthetic Research Department, ASKA Pharmaceutical Co., Ltd.

• HAYASHI Hiroyuki

  Synthetic Research Department, ASKA Pharmaceutical Co., Ltd.

• YAMAUCHI Yukinao

  Pharmacological Research Department, ASKA Pharmaceutical Co., Ltd.

• Asagarasu Akira

  Synthetic Research Department Aska Pharmaceutical Co. Ltd.

• Yamauchi Yukinao

  Pharmacological Research Department Aska Pharmaceutical Co. Ltd.

• Hayashi Hiroyuki

  Synthetic Research Department Aska Pharmaceutical Co. Ltd.

関連論文

• Antitumor Activity of TZT-1027, a Novel Dolastatin 10 Derivative
• Design and Synthesis of Piperazinylpyridine Derivatives as Novel 5-HT_ Agonists/5-HT_3 Antagonists for the Treatment of Irritable Bowel Syndrome (IBS)
• Design and Synthesis of Piperazinylpyridine Derivatives as Novel 5-HT_ Agonists/5-HT_3 Antagonists for the Treatment of Irritable Bowel Syndrome (IBS)

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