Studies on biologically Active Halogenated Compounds. II. Chemical Modifications of 6-Amino-2-fluoromethyl-3-(o-tolyl)-4 (3H)-quinazolinone and the CNS Depressant Activities of Related Compounds
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概要
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A number of derivatives of 6-amino-2-fluoromethyl-3-(o-tolyl)-4 (3H)-quinazolinone (15), a potent muscle relaxant, have been prepared and screened in terms of the loss of righting reflex test and the rotating rod test in mice. Several derivatives with additional fluorine substitution or with repositioning of the fluorine atom exhibited high activities. Other structural modifications included acylation, carbamoylation, and alkoxycarbonylation of the 6-amino group, hydroxylation at the 3-tolyl group, and replacement of the fluorine atom at the 2-fluoromethyl group by oxygen, nitrogen, and sulfur nucleophiles ; these modifications all resulted in loss of activity.
- 公益社団法人日本薬学会の論文
- 1979-11-25
著者
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石田 柳一
Research Laboratory of Applied Biochemistry, Tanabe Seiyaku Co., Ltd.
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井上 一三
Research Laboratories of Tanabe Seiyaku Co., Ltd.
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大稲 豊生
Research Laboratory of Applied Biochemistry, Tanabe Seiyaku Co., Ltd.
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山田 義久
Research Laboratory Of Applied Biochemistry Tanabe Seiyaku Co. Ltd.
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谷 醇一
Research Laboratory of Applied Biochemistry, Tanabe Seiyaku Co., Ltd.
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落合 喬
Research Laboratories of Tanabe Seiyaku Co., Ltd.
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井上 一三
Research Laboratories Of Tanabe Seiyaku Co. Ltd.
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井上 一三
Department Of Synthetic Chemistry Research Laboratory Of Applied Biochemistry Tanabe Seiyaku Co. Ltd
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大稲 豊生
Research Laboratory Of Applied Biochemistry Tanabe Seiyaku Co. Ltd.
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石田 柳一
田辺製薬安全性研
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石田 柳一
Research Laboratories of Tanabe Seiyaku Co., Ltd.
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