Diamine Derivatives Containing Imidazolidinylidene Propanedinitrile as a New Class of Histamine H3 Receptor Antagonists: Conformationally Restricted Derivatives

• Sasho Setsuya

  Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co., Ltd.

• Seishi Takashi

  Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co., Ltd.

• Kawamura Mariko

  Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co., Ltd.

• Tomuro Misato

  Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co., Ltd.

• Hirose Ryo

  Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co., Ltd.

• Toki Shinichiro

  Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co., Ltd.

• Shimada Junich

  Medicinal Chemistry Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co., Ltd.

抄録

Novel conformationally restricted diamine derivatives containing imidazolidinylidene propanedinitrile were synthesized and evaluated for human and rat histamine H₃ receptor (H₃R) binding affinities. Among them, compounds 2b, 2c, 2j, 2k and 2m were found to be potent ligands for both H₃Rs with K_i values in the sub-nanomolar range, and showed potent H₃ receptor antagonism.

収録刊行物

• ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ

  ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 57 (3), 288-293, 2009

  公益社団法人 日本薬学会

キーワード

• histamine H₃ receptor
• antagonist
• imidazolidinylidene propanedinitrile
• diamine

詳細情報

• CRID: 1390001204168427648
• NII論文ID: 110007122354
• NII書誌ID: AA00602100
• DOI: 10.1248/cpb.57.288
• ISSN: 13475223
• ISSN: 00092363
• NDL書誌ID: 10166866
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I10166866
• Web Site: http://www.jstage.jst.go.jp/article/cpb/57/3/57_3_288/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2009201620
• 本文言語コード: en
• データソース種別:
  • JaLC
  • NDL
  • Crossref
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可