title: Design, synthesis and biological activity evaluation of arylpiperazine derivatives for the treatment of neuropathic pain.
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.
authors: Department of Systems Biology, Huazhong University of Science and Technology, 1037 Luoyu Road, Wuhan 430074, China.
authors: Yin
authors: Y
authors: Chen
authors: Guan
authors: G
authors: Wang
authors: Xiangqing
authors: X
authors: Xu
authors: Bi-Feng
authors: BF
authors: Liu
authors: Jianqi
authors: J
authors: Li
authors: Guisen
authors: G
authors: Zhang
mesh_terms: D000700:Analgesics / Q000627:therapeutic use*; D000818:Animals; D051379:Mice; D009437:Neuralgia / Q000188:drug therapy*; D000077489:Piperazine; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D000700:Analgesics; D010879:Piperazines; D000077489:Piperazine