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具有抗炎和镇痛活性的1-取代-5-二烷基氨基甲基-1,5,6,7-四氢吲唑-4-酮

1-substituted 5-dialkylaminomethyl-1,5,6,7-tetrahydroindazol-4-ones with antiinflammatory and analgesic activity.

作者信息

Mosti L, Menozzi G, Schenone P, Tortora G, di Mauro G, Lama M, Marmo E

出版信息

Farmaco Sci. 1987 Apr;42(4):259-66. doi: 10.1002/chin.198744184.

Abstract

The synthesis of 1-phenyl- and 1-methyl-5-dialkylamino-methyl-1,5,6,7-tetrahydroindazol-4-ones (III) and (IV) by Mannich reaction of the corresponding 1-substituted 1,5,6,7-tetrahydroindazol-4-ones (I) and (II) is described. Some compounds (III) showed a good antiinflammatory and analgesic activity in rats and mice, respectively. Infiltration anesthesia in mice and antiacetylcholine activity in vitro are also reported.

摘要

描述了通过相应的1-取代的1,5,6,7-四氢吲唑-4-酮(I)和(II)的曼尼希反应合成1-苯基-和1-甲基-5-二烷基氨基甲基-1,5,6,7-四氢吲唑-4-酮(III)和(IV)。一些化合物(III)分别在大鼠和小鼠中显示出良好的抗炎和镇痛活性。还报道了在小鼠中的浸润麻醉和体外抗乙酰胆碱活性。

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