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

Yin Chen 1 , Guan Wang 2 , Xiangqing Xu 3 , Bi-Feng Liu 1 , Jianqi Li 2  and Guisen Zhang 1,3,* email
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; in revised form: 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

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Cite This Article

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.

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