Azabicycloalkanes as Analgetics. VII. 1-Phenyl-3-azabicyclo [3. 3. 1] nonanes
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概要
- 論文の詳細を見る
As part of study on the structure-activity relationships of phenylazabicycloalkane analgetics, the title compound (I) has been synthesized. Structure (I) could be regarded as a piperidine analog of 1-phenyl-6-azabicyclo [3. 2. 1] octane (II), a known partial agonist, and also as a conformationally constrained analog of the 3-phenyl-piperidine analygetics (XIX). From the keto ester (III), I was obtained by the sequence of reactions outlined in Chart 2. Neither by the AcOH writhing nor by the hot-plate method, I exhibited appreciable analgetic activity. In contrast, the N-methyl compounds (XIV and XV) showed narcotic antagonist activity, with the former being the more active. Replacement of the N-methyl group of XV by a propyl and an allyl group (XVIIIa, d) resulted in an increase in the antagonist activity. Their activity was about one-tenth that of nalorphine.
- 公益社団法人日本薬学会の論文
- 1977-07-25
著者
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川森 政敏
Organic Chemistry Research Laboratory
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武田 幹男
Research Laboratories, Tanabe Seiyaku, Co., Ltd.
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塗本 精一
Safety Research Laboratory Tanabe Seiyaku Co. Ltd.
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塗本 精一
Research Laboratories, Tanabe Seiyaku Co., Ltd.
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武田 幹男
Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd.
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野口 勝通
Organic Chemistry Research Laboratory Tanabe Seiyaku Co. Ltd. :(present Address)sapporo Branch Tanab
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