2-(E)-亚苄基-5-氨甲基环戊醇类化合物的合成及抗炎活性研究

Synthesis and anti-inflammatory activity of 2-(E)-benzylidene-5-aminomethylcyclopentanols

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.