ピリダジノン誘導体の研究(第16報)3(2H)-ピリダジノン誘導体の合成と鎮痛消炎作用 Studies on Pyridazinone Derivatives. XVI. Analgesic-Antiinflammatory Activities of 3 (2H)-Pyridazinone Derivatives

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Abstract

In order to examine analgesic and antiinflammatory activities of the position isomers of 4-ethoxy-2-methyl-5-morpholino-3 (2H)-pyridazinone (1, emorfazone), an analgesic-antiinflammatory drug, 5-ethoxy-2-methyl-4-morpholino-3 (2H)-pyridazinone (2), 6-ethoxy-2-methyl-4-morpholino-3 (2H)-pyridazinone (3) and 6-ethoxy-2-methyl-5-morpholino-3 (2H)-pyridazinone (4) were prepared. Since 4 showed the most strong activity among the compounds tested, various 6-alkoxy- or 2-cyclohexyl- or 2-phenyl-5-substituted amino-3 (2H)-pyridazinones (15, 16) were prepared and examined for their activities. As a result, 4 and 2-methyl-5-morpholino-6-n-propoxy-or 6-n-butoxy-3 (2H)-pyridazinone (15b, c) and 6-ethoxy-2-ethyl-5-morpholino-3 (2H)-pyridazinone (151) were revealed to be more potent in analgesic and antipyretic activities than commercial drugs (1, aminopyrine, mepirizole, tiaramide HCl, phenylbutazone, mefenamic acid). On the basis of the available data, the structure-activity relationship in a series of 6-alkoxy-2-alkyl-5-substituted amino-3 (2H)-pyridazinones (15, 16) was also discussed.

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 114(2), 94-110, 1994

    The Pharmaceutical Society of Japan

Codes

  • NII Article ID (NAID)
    110003649471
  • NII NACSIS-CAT ID (NCID)
    AN00284903
  • Text Lang
    UNK
  • ISSN
    0031-6903
  • NDL Article ID
    3872195
  • NDL Source Classification
    SD0(薬学)
  • NDL Source Classification
    ZS51(科学技術--薬学)
  • NDL Call No.
    Z19-411
  • Data Source
    NDL  NII-ELS  J-STAGE 
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