Design, synthesis, and biological evaluation of the N-diarylalkenyl-piperidinecarboxylic acid derivatives as GABA uptake inhibitors (I)

J Zheng, R Wen, X Luo, G Lin, J Zhang, L Xu…

文献索引：Zheng, Jianbin; Wen, Ren; Luo, Xiaomin; Lin, Guoqiang; Zhang, Jiange; Xu, Linfeng; Guo, Lihe; Jiang, Hualiang Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 1 p. 225 - 227

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被引用次数: 14

摘要

Twenty novel N-diarylalkenyl-piperidinecarboxylic acid derivatives were synthesized and evaluated as γ-aminobutyric acid uptake inhibitors. The biological assay showed that (R)-1- [4, 4-bis (3-phenoxymethyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic hydrochloride (4e) possessed almost as strong GAT1 inhibitory activity as tiagabine. The synthesis and structure–activity relationships are discussed.