摘要
目的设计合成2-(E)-亚苄基-5-氨甲基环戊醇类化合物,并对其抗炎活性进行初步的评价。方法以环戊酮为起始原料,通过Stork烯胺反应、Mannich反应、选择性还原制备目标化合物;以二甲苯致小鼠耳肿胀模型测试目标化合物的抗炎活性。结果共合成了12个新化合物,经1H-NMR、MS和IR确证结构。初步药理实验结果显示10个目标化合物具有较强的抗炎活性。结论目标化合物稳定性有所提高并且保留了抗炎活性。
Aim To synthesize 2-(E )-benzylidene-5-aminomethylcyclopentanols and study their anti-inflammatory activity. Methods The target compounds were synthesized from cyclopentanone via Stork reaction, Mannich reaction and selective reduction. Xylene-induced mice ear edema assay was used to evaluate the antiinflammatory activity of the target compounds. Results Twelve novel compounds were synthesized and characterized using ^1H-NMR, MS and IR. Preliminary pharmacological test showed that ten target compounds possessed potent anti-inflammatory activity. Conclusion The stability of the target compounds is improved and the anti-inflammatory activity is maintained.
出处
《中国药物化学杂志》
CAS
CSCD
2006年第4期198-201,共4页
Chinese Journal of Medicinal Chemistry
基金
教育部高等学校博士学科点专项科研基金项目(20040163001)
辽宁省自然科学基金项目(20032044)