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

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

1
Department of Systems Biology, Huazhong University of Science and Technology, 1037 Luoyu Road, Wuhan, 430074, China
2
Shanghai Institute of Pharmaceutical Industry, 1111 North Zhongshan Road, Shanghai, 200437, China
3
Jiangsu Nhwa Pharmaceutical Corporation, Ltd. 69# Minzhu South Road Xuzhou City, Jiangsu, 221009, China
*
Author to whom correspondence should be addressed.
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 (CC BY 3.0).

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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.

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