2-(E)-亚苄基-5-芳氨基甲基环戊醇类化合物的合成及其抗炎活性研究

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

目的设计合成2-(E)-亚苄基-5-芳氨基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缩合反应、胺交换反应和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16个新化合物,其结构经1H-NMR和MS谱确证。结论初步药理实验结果显示,4个目标化合物具有较强的抗炎活性。

Aim 2- （E）-benzylidene-5-arylaminomethylcyclopentanols were synthesized and their anti-inflam- matory activity was studied. Methods The target compounds were synthesized from cyclopentanone via Stork reaction, Mannich condensation, amine exchange and selective reduction. Xylene-induced mice ear edema assay was used to evaluate their anti-inflammatory activity. Results Sixteen novel compounds were synthesized and characterized by ^1 H-NMR and MS. Conclusion Preliminary pharmacological test show that four compounds possess potent anti-inflammatory activity.