A series of 7-substitued-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-one(1a-p)were synthesized and evaluated the anti-inflammatory activity via the method of the xylene-induced ear edema in mice.Among them,three compounds were demonstrated more effective anti-inflammatory activity than the reference anti-inflammatory drug indomethacin.7-(4-methoxyphenoxy)-[1,2,4] triazolo[1,5-a]pyrimidin-5(4H)-one(1k)exhibited the potent anti-inflammatory activity and 70.71%inhibition at dose of 100 mg ·kg-1(30 min after i.p administration),it was worth studying further.%本文设计合成一系列7-取代-[1,2,4]三唑[1,5-a]嘧啶-5(4H)-酮(1a-p)类衍生物,并用小鼠耳肿胀法测定其抗炎活性.其中,在100 mg·kg-1剂量下,三个化合物的抗炎活性优于阳性对照药吲哚美辛,而化合物7-(4-甲氧基苯基)-[1,2,4]三唑[1,5-a]嘧啶-5(4H)-酮(1k)表现出最强的抗炎活性,其耳肿胀抑制率为70.71%,具有进一步研究的价值.
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