Molecules 2011, 16(7), 5785-5806; doi:10.3390/molecules16075785
Article

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

Received: 7 April 2011; in revised form: 24 June 2011 / Accepted: 27 June 2011 / Published: 7 July 2011
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Abstract: 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.
Keywords: arylpiperazine; antinociceptive; neuropathic pain; spared nerve injury; chronic constriction injury
PDF Full-text Download PDF Full-Text [391 KB, uploaded 18 June 2014 19:39 CEST]

Export to BibTeX |
EndNote


MDPI and ACS Style

Chen, Y.; Wang, G.; Xu, X.; Liu, B.-F.; Li, J.; Zhang, G. Design, Synthesis and Biological Activity Evaluation of Arylpiperazine Derivatives for the Treatment of Neuropathic Pain. Molecules 2011, 16, 5785-5806.

AMA Style

Chen Y, Wang G, Xu X, Liu B-F, Li J, Zhang G. Design, Synthesis and Biological Activity Evaluation of Arylpiperazine Derivatives for the Treatment of Neuropathic Pain. Molecules. 2011; 16(7):5785-5806.

Chicago/Turabian Style

Chen, Yin; Wang, Guan; Xu, Xiangqing; Liu, Bi-Feng; Li, Jianqi; Zhang, Guisen. 2011. "Design, Synthesis and Biological Activity Evaluation of Arylpiperazine Derivatives for the Treatment of Neuropathic Pain." Molecules 16, no. 7: 5785-5806.

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert