Psychotropic Agents. II. Synthesis and Psychotropic Activity of conformationally Restricted Butyrophenone Analogs

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概要

• 論文の詳細を見る

• 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.

• 公益社団法人日本薬学会の論文
• 1979-01-25

著者

• 佐藤 誠

  Faculty of Pharmaceutical Sciences Toyama Medical and Pharmaceutical University

• 小島 浩

  Research Institute Daiichi Seiyaku Co. Ltd.

• 佐藤 誠

  Research Institute, Daiichi Seiyaku Co., Ltd.,

• 内丸 文彦

  Research Institute, Daiichi Seiyaku Co., Ltd.

• 山崎 輝清

  Research Institute, Daiichi Seiyaku Co., Ltd.

• 北川 正之

  Research Institute, Daiichi Pharmaceutical Co., Ltd.,

• 上野 勝次郎

  Research Institute, Daiichi Seiyaku Co., Ltd.

• 内丸 文彦

  Research Institute Daiichi Seiyaku Co. Ltd.

• 上野 勝次郎

  Research Institute Daiichi Seiyaku Co. Ltd.

• 北川 正之

  Research Institute Daiichi Pharmaceutical Co. Ltd.

• 山崎 輝清

  Research Institute Daiichi Seiyaku Co. Ltd.

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