7-取代-[1,2,4]三唑[1,5-a]嘧啶-5(4H)-酮衍生物的合成及抗炎活性的研究  

Synthesis and anti-inflammation activity of 7-substitued-[1,2,4] triazolo [1,5-a] pyrimidin-5(4H)-one derivatives

作　　者：周勇 张洪健 尹秀梅[2] ZHOU Yong;ZHANG Hongjian;YIN Xiumei(The Affiliated Hospital of Chongqing Three Gorges Medical College,Chonqing 4041202,China;College of Pharmacy, Yanbian University,Yanji 133002 ,China)

机构地区：[1]重庆三峡医药高等专科学校附属医院,重庆404120 [2]延边大学药学院,吉林延吉133002

出　　处：《化学研究与应用》2018年第2期196-200,共5页Chemical Research and Application

基　　金：国家自然科学基金项目(81360468)资助

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 of7-substitued-[1,2,4]triazolo[1,5-a]pyrimidin-5(4^)-one(la-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(4^)-one(lk)exhibited the potent anti-inflammatory activity and70.71%inhibition at dose of100mg?kg1(30min after i.p administration),t was worth studying further.

关 键 词：合成 三唑 嘧啶 抗炎 耳肿胀模型 

分 类 号：O626.41[理学—有机化学]