Design, Synthesis and Biological Activity Evaluation of Arylpiperazine Derivatives for the Treatment of Neuropathic Pain

Molecules

Yin Chen¹  Guan Wang¹  Xiangqing Xu¹  Bi-Feng Liu¹  Jianqi Li¹ 

[1] ¹Department of Systems Biology, Huazhong University of Science and Technology, 1037 Luoyu Road, Wuhan, 430074, China ²Shanghai Institute of Pharmaceutical Industry, 1111 North Zhongshan Road, Shanghai, 200437, China ³Jiangsu Nhwa Pharmaceutical Corporation, Ltd. 69# Minzhu South Road Xuzhou City, Jiangsu, 221009, China

关键词: arylpiperazine;    antinociceptive;    neuropathic pain;    spared nerve injury;    chronic constriction injury;   

DOI  :  10.3390/molecules16075785

来源: mdpi

【 摘 要 】

In this work, a series of arylpiperazine derivatives were synthesized and screened by in vivo pharmacological trials. Among the tested compounds, 2-(4-(3-(trifluoromethyl)phenyl)piperazin-1-yl)-1-phenylethanone (18) and 2-(4-(2,3-dimethylphenyl)piperazin-1-yl)-1-phenylethanone (19) exhibited potent analgesic activities in both the mice writhing and mice hot plate tests. They showed more than 70% inhibition relative to controls in the writhing test, and increased latency by 116.0% and 134.4%, respectively, in the hot plate test. Furthermore, compound 18 was also active in the models of formalin pain and neuropathic pain without sedative side effects.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.