Anti-inflammatory, analgesic properties and antipyretic action of 3-aminoindazole derivatives

Abstract

We reported an interesting anti-inflammatory effect of one of 3-aminoindazole derivatives in the proceeding paper. We wish to report the anti-inflammatory, analgesic and antipyretic effect of 3-aminoindazole derivatives. Several new derivatives of 3-aminoindazole were synthesized. They were examined for their anti-inflammatory effect by the method of anti-inflammatory assays by using carrageenin edema, dextran edema, serotonin edema, histamine edema and bradykinin edema. The analgesic effect in mice was examined by using the acetic acid writhing test and the antipyretic effect in rats was examined with yeast. 3-(3-Morpholinopropylamino) indazole which is a representative compound was found to possess three times more effective anti-inflammatory property with the carrageenin edema than the reference drug, tiaramide and the same analgesic property as tiaramide. 3-(3-Morpholinopropylamino) indazole is thought to possess different mechanism of acidic non-steroidal anti-inflammatory drugs such as indomethacin and mefenamic acid because this compound inhibited the hind paw edema induced with histamine, serotonin, bradykinin and dextran. It was found that this compound at 50mg/kg, p.o. was as effective in its antipyretic action as indomethacin at 10mg/kg, p.o. Among other 15 new derivatives, 3-[3-(2, 6-dimethylpiperidino) propylamino] indazole was also found to possess a similar degrees of anti-inflammatory, analgesic and antipyretic effect as 3-(3-morpholinopropylamino) indazole.