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.
作者
周勇
张洪健
尹秀梅
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)
出处
《化学研究与应用》
CAS
CSCD
北大核心
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
关键词
合成
三唑
嘧啶
抗炎
耳肿胀模型
synthesis
triazole
pyrimidine
anti-inflammation
ear edema model
