Synthesis and protein tyrosine kinases inhibitory activity of substituted benzyl piperazine derivatives
10.13220/j.cnki.jipr.2018.01.010
- VernacularTitle:取代苄基哌嗪类化合物的合成及其蛋白酪氨酸激酶抑制活性的研究
- Author:
Sheng-Hua HAN
1
;
Hong-Yan LIU
;
Hai-Rong ZHANG
;
Peng-Fei MA
Author Information
1. 山西大同大学化学与环境工程学院
- Keywords:
piperazine;
synthesis;
protein tyrosine kinases(PTK);
activity
- From:
Journal of International Pharmaceutical Research
2018;45(1):57-60
- CountryChina
- Language:Chinese
-
Abstract:
Objective Using substituted benzyl piperazine as the raw material to design and synthesize new piperazine deriva-tives with protein tyrosine kinase(PTK)inhibitory activity. Methods Benzoic acid was used as starting compound to synthesize a key intermediate,2-chloroethyl benzoate,and the target compounds were synthesized by further reaction of the key intermediate with different substituted benzyl piperazine derivatives.Enzyme-linked immunosorbent assay(ELISA)was used to test the PTK inhibitory activity of the compounds.Results Fifteen new compounds were synthesized and their structures were verified by IR,1H NMR,MS, and elemental analysis.The PTK inhibitory activity of 3h and 3o was stronger than that of the other compounds.Conclusion The syn-thetic method is simple,and the raw materials are cheap and readily available.Compounds 3h and 3o showed relatively higher PTK in-hibitory activities.
