Design, synthesis, and biological evaluation of the N-diarylalkenyl-piperidinecarboxylic acid derivatives as GABA uptake inhibitors (I) |
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| Authors: | Zheng Jianbin Wen Ren Luo Xiaomin Lin Guoqiang Zhang Jiange Xu Linfeng Guo Lihe Jiang Hualiang |
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| Institution: | Department of Medicinal Chemistry, Fudan University, Shanghai 200032, China. |
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| Abstract: | Twenty novel N-diarylalkenyl-piperidinecarboxylic acid derivatives were synthesized and evaluated as gamma-aminobutyric acid uptake inhibitors. The biological assay showed that (R)-1-4,4-bis(3-phenoxymethyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic hydrochloride possessed almost as strong GAT1 inhibitory activity as tiagabine. The synthesis and structure-activity relationships are discussed. |
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