Synthesis and Histamine H_2-Antagonist Activity of 4-Quinazolinone Derivatives
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概要
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With the aim of developing new atiulcer agents, a series of 4-quinazolinone derivatives was synthesized and tested for histamine H_2-antagonist activity and gastric antisecretory activity. Thus, 2-alkylamino- (8a-d, 10a-s), 2-alkylthio- (15), and 2-alkyl-4-quinazolinones (18a-k) were prepared by the condensation of alkylamines with 2-chloro- or 2-methlthio-4-quinazolinones, the condensation of alkyl bromides with 2-mercapto-4-quinazolinones, and the condensation of alkylcarboxylic acids with anthranilamides, respectively.Several of the 4-quinazolinone derivatives thus synthesized showed potent H_2-antagonist activity, and one of them, 2-[3-[3-(1-piperidinylmehyl)phenoxy]propylamino]-4(3H)-quinazo-linone (8d) showed the most potent antisecretory activity. The structure-activity relationships are discussed.
- 社団法人日本薬学会の論文
- 1988-08-25
著者
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加藤 日出男
北陸製薬株式会社
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小川 信男
北陸製薬株式会社中央研究所研究開発本部
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小川 信男
Research and Development Division, Hokuriku Seiyaku Co., Ltd.,
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越中 栄一
Research and Development Division, Hokuriku Seiyaku Co., Ltd.,
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加藤 日出男
Research and Development Division, Hokuriku Seiyaku Co., Ltd.,
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伊藤 安夫
Research and Development Division, Hokuriku Seiyaku Co., Ltd.,
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吉田 敏彦
北陸製薬株式会社中央研究所
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吉田 敏彦
Research Laboratories, Hokuriku Seiyaku Co., Ltd.,
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荒谷 隆幸
Research Laboratories, Hokuriku Seiyaku Co., Ltd.,
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越中 栄一
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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伊藤 安夫
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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加藤 日出男
北陸製薬株式会社中央研究所
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荒谷 隆幸
Research Laboratories Hokuriku Seiyaku Co. Ltd.
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