Structure-Activity Relationship of 3- and 4-Acyloxy-1-(1,3-dioxolan-4-ylmethyl) piperidine Derivatives
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概要
- 論文の詳細を見る
Derivatives of 3- and 4-acyloxy-1-(1,3-dioxolan-4-ylmethyl) piperidine were synthesized and tested for atropine-like activities on the ileum from guinea pigs. The structure-activity relationship was assessed. Features favoring potent atropine-like action were considered to be as follows : (1) both the acyloxy group and the dioxolane ring should be diequatorial on the piperidine ring, (2) the acyloxy group should be moderately bulky, and (3) a substituent on the dioxolane ring is unnecessary. The highest activity (pA_2) determined was 8.64 which is about 50 times that of scopolamine N-butyl bromide.
- 社団法人日本薬学会の論文
- 1985-02-25
著者
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長谷川 賀洋
Research Institute for Biology & Chemistry, Tsumura Co., Ltd.,
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内藤 泰男
Research Laboratories Ohta Pharmaceutical Co. Ltd.
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川田 登美枝
Research Laboratories Ohta Pharmaceutical Co. Ltd.
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梶原 良夫
Research Laboratories Ohta Pharmaceutical Co. Ltd.
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高柳 一成
東邦大学薬学部
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吉田 誠一郎
Research Laboratories, Ohta Pharmaceutical Co., Ltd.
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菅井 三郎
Research Laboratories, Ohta Pharmaceutical Co., Ltd.
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神原 俊文
Research Laboratories, Ohta Pharmaceutical Co., Ltd.
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赤星 三弥
Research Laboratories, Ohta Pharmaceutical Co., Ltd.
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久津間 輝雄
Research Laboratories, Ohta Pharmaceutical Co., Ltd.
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伊川 博
Research Laboratories, Ohta Pharmaceutical Co., Ltd.
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勝原 徳寛
Research Laboratories, Ohta Pharmaceutical Co., Ltd.
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寺脇 康文
Research Laboratories, Ohta Pharmaceutical Co., Ltd.
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高柳 一成
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences
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赤星 三彌
Research Laboratories, Ohta Pharmaceutical Co., Ltd.,
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高柳 一成
東邦大学
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高柳 一成
Department Of Chemical Pharmacology Toho University School Of Pharmaceutical Sciences
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赤星 三彌
Research Laboratories Ohta Pharmaceutical Co. Ltd.
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長谷川 賀洋
Research Laboratories Ohta Pharmaceutical Co. Ltd.
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久津間 輝雄
Research Laboratories Ohta Pharmaceutical Co. Ltd.:(present Address) Research Laboratories Fujirebio
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伊川 博
Central Research Laboratories Fujirebio Inc.
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吉田 誠一郎
Research Laboratories Ohta Pharmaceutical Co. Ltd.
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寺脇 康文
Research Laboratories Ohta Pharmaceutical Co. Ltd.
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菅井 三郎
Research Laboratories Ohta Pharmaceutical Co. Ltd.
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神原 俊文
Research Laboratories Ohta Pharmaceutical Co. Ltd.
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勝原 徳寛
Research Laboratories Ohta Pharmaceutical Co. Ltd.:(present Address) Dojindo Co.
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高柳 一成
Department of chemical Pharmacdogy, Faculty of Pharmaceutical Sciences, University of Tokyo
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