Psychotropic agents. II. Synthesis and psychotropic activity of conformationally restricted butyrophenone analogs.

• 佐藤 誠

• 北川 正之

• 内丸 文彦

• 上野 勝次郎

• 小島 浩

• 山崎 輝清

抄録

In order to search for new psychotropic agents, several conformationally restricted analogs (see Chart 1D) of haloperidol or benperidol were synthesized. cis-and trans-1-[2- (2-Phenylcyclopropyl) ethyl] piperidine derivatives (Xa, Xb, and XXIV) were prepared in several steps from the corresponding cis-and trans-1-phenyl-1-butene derivatives (III and XX). The effect of the compounds on spontaneous motor activity in mice was determined. trans-Isomer (Xb), which was the most active compound, was about 11 times more active than cis-isomer (XXIV). But the activity of Xb was about one-fifth as potent as benperidol. Structure-activity relationships of these compounds are discussed.

収録刊行物

• ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ

  ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 27 (1), 119-128, 1979

  公益社団法人 日本薬学会

キーワード

• 1-butyne derivatives

詳細情報

• CRID: 1390282679145089536
• NII論文ID: 110003623416
• NII書誌ID: AA00602100
• DOI: 10.1248/cpb.27.119
• ISSN: 13475223
• ISSN: 00092363
• PubMed: 34487
• Web Site: http://www.jstage.jst.go.jp/article/cpb1958/27/1/27_1_119/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/1980035461
• 本文言語コード: en
• データソース種別:
  • JaLC
  • Crossref
  • PubMed
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可