摘要
目的:研究具有咪唑并[1,2-a]嘧啶结构化合物的合成和抗炎活性。方法:在咪唑并[1,2-a]嘧啶的结构基础上,合成2-位和3-位上有两个芳香性取代基的咪唑并[1,2-a]嘧啶类化合物(5a～5o),并对所合成的化合物进行二甲苯诱导的小鼠耳肿胀模型抗炎活性实验。结果:合成的15个未见报道的目标化合物结构经元素分析,红外光谱、核磁共振氢谱、质谱确证;初步生物活性测试表明,多数化合物具有不同程度的抗炎活性,其中化合物5d,5f和5l的活性较好。结论:与布洛芬相比,咪唑并[1,2-a]嘧啶类化合物能保持中等的抗炎活性,2-位和3-位被两个相邻的芳基取代可以改善COX-2的抑制作用。
Aim： To synthesize and characterize a series of imidazo[ 1,2-a] pyrimidine derivatives, and to evaluate their anti-inflammatory activities. Methods： Based on the analysis of the structure of imidazo[ 1,2-a] pyrimidine, a series of compounds （5a-5o） substituted adjacently with two aryls at positions 2 and 3 were designed and synthesized. Their anti-inflammatory activities were evaluated by means of xylene-induced ear swelling in mice. Results： Their structures were confirmed by ^1H NMR, IR, MS and elemental analysis. It was found that most of the synthesized compounds possessed the anti-inflammatory activity, of which compound 5d, 5f and 5I showed the most potent activity. Conclusion： Imidazo[ 1,2-a] pyrimidine compounds keep moderate anti-inflammatory activities as compared with that of ibuprofen.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2009年第1期16-20,共5页
Journal of China Pharmaceutical University
基金
国家自然科学基金资助项目(No.30772647)~~
