摘要
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。
A series of 7-substitued-[1,2,4]triazolo[1,5-a]pyrimidin-5( 4 H)-one( 1 a-p) were synthesized and evaluated the antiinflammatory 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( 4 H)-one( 1 k) 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.
引文
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