N-[3-(2-呋喃基)丙烯酰基]-N'-取代苄基哌嗪类化合物的合成与生物活性研究

Synthesis and biological activity of N-[3-( 2-furanyl)-acryloyl]-N'-substituted benzyl piperazine derivatives

目的合成了N-3-[（2-呋喃基）丙烯酰基]-N＇-取代基哌嗪类化合物,并对其进行生物活性的初步测试。方法以呋喃丙烯酸为原料,与不同的取代苄基哌嗪反应,得到一系列哌嗪类化合物;通过MTT法,测定目标化合物对血清诱导的血管平滑肌细胞增殖的抑制活性。结果与结论合成了12个未见文献报道的化合物,所有化合物的结构均经IR、~1H-NMR、EA和MS确证;活性测试结果表明,化合物5d、5e、5f、5g、5h、5i具有一定的血管平滑肌细胞增殖抑制活性。

A series of N- [ 3- （ 2-furanyl ） -acryloyl ] -N＇-substituted benzyl piperazine derivatives were synthe- sized and evaluated for their inhibitory activities on vascular smooth muscle cell（VSMC） proliferation. The target compounds could be obtained by direct condesation of furylacrylic acid with different substituted ben- zyl piperazine derivatives. Tweleve new compounds were verified by IR, I H-NMR, MS and elemental analy- sis. The inhibitory effect of the target compounds on VSMC proliferation was investigated by MTT. The compounds 5d ,5e ,5f,5g ,5h and 5i showed the moderate inhibitory activities.