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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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.
- YAKUGAKU ZASSHI
YAKUGAKU ZASSHI 114(2), 94-110, 1994
The Pharmaceutical Society of Japan