Syntheses of Monocyclic and Bicyclic 2,4-(1H, 3H)-Pyrimidinediones and Their Serotonin 2 Antagonist Activities

書誌事項

公開日
1990-10-25
公開者
公益社団法人日本薬学会

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説明

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.

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詳細情報 詳細情報について

  • CRID
    1573387452274548992
  • NII論文ID
    110003628139
  • NII書誌ID
    AA00602100
  • ISSN
    00092363
  • 本文言語コード
    en
  • データソース種別
    • CiNii Articles

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