Synthesis and inhibitory activities on vascular smooth muscle cell proliferation of furan-acrylic acyl group piperazine derivatives / 中国生化药物杂志

ABSTRACT

Objective To synthesis,nine N-[3-(2-furanyl)-acryloyl]-N'-substituted benzyl piperazine derivatives were synthesized and evaluated for their primary biological activities.Methods First, the furylacrylic acid was synthesized, Then the target compounds could be obtained by direct furylacrylic acid with the different substituted benzyl piperazine derivatives.In the biological active experiments, taking the different concentrations, comparing with the blank test, the inhibitory effect of the target compounds on VSMC proliferation was investigated by MTT.Results The successful synthesis of nine new compounds.The method was mild and get high yields.The structures of these compounds were confirmed by IR 1 H-NMR, MS, and elemental analysis.The results of preliminary activity test showed that the synthesized products exhibited inhibitory activity at different concentrations , and the highest inhibitory rate was 15μg/mL.Pharmacological results showed that the compounds 3e, 3f and 3 g showed the moderate inhibitory activities against vascular smooth muscle cells proliferation were higher than other compounds , and were worth further studying.Conclusion The synthesized compounds have inhibitory activities and could very well lead to the development of novel types of treat atherosclerosis drug .