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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

1, 2, 3, 1, 2 and 1,3,*
Received: 7 April 2011 / Revised: 24 June 2011 / Accepted: 27 June 2011 / Published: 7 July 2011
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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 arylpiperazine; antinociceptive; neuropathic pain; spared nerve injury; chronic constriction injury
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.

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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.

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