Syntheses of Monocyclic and Bicyclic 2,4-(1H, 3H)-Pyrimidinediones and Their Serotonin 2 Antagonist Activities
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概要
- 論文の詳細を見る
New serotonine 2(5-HT_2) antagonists with a monocyclic or bicyclic 2,4(1H, 3H)-pyrimidinedione have been prepared and their activities evaluated. In a series of monocyclic compounds, 1-substituted 5-phenyl-2,4(1H, 3H)-pyrimidinedione 14 showed potent in vitro activity, and the corresponding 3-substituted 5-phenyl and 6-phenyl derivatives 3,8 and 20a also showed moderate activity. In the bicyclic compounds, 3-substituted 5,6,7,8-tetrahydro-2,4(1H, 3H)-quinazolinedione 33 exhibited the most potent activity among the compounds prepared in this paper. The in vivo antagonist activity of 33 was comparable of that of ketanserin, a typical peripheral 5-HT_2 antagonist.
- 公益社団法人日本薬学会の論文
- 1990-10-25
著者
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渡辺 好文
Daiichi Pharmaceutical Co. Ltd. Research Institute
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碓井 博幸
Daiichi Pharmaceutical Co., Ltd.,
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金尾 宗史
Daiichi Pharmaceutical Co., Ltd.,
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芝野 俊郎
Daiichi Pharmaceutical Co., Ltd., Research Institute
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田中 剛
Daiichi Pharmaceutical Co., Ltd., Research Institute
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碓井 博幸
Daiichi Pharmaceutical Co. Ltd.
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田中 剛
Daiichi Pharmaceutical Co. Ltd. Research Institute
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金尾 宗史
Daiichi Pharmaceutical Co. Ltd.
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芝野 俊郎
Daiichi Pharmaceutical Co. Ltd. Research Institute
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