Title of article
Design, synthesis, and biological evaluation of the N-diarylalkenyl-piperidinecarboxylic acid derivatives as GABA uptake inhibitors (I)
Author/Authors
Jianbin Zheng، نويسنده , , Ren Wen، نويسنده , , Xiaomin Luo، نويسنده , , Guoqiang Lin، نويسنده , , Jiange Zhang، نويسنده , , Linfeng Xu، نويسنده , , Lihe Guo، نويسنده , , Hualiang Jiang and Helmut Grubmüller، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
3
From page
225
To page
227
Abstract
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.
Keywords
GABA uptake inhibitors , GAT1 , Antiepileptic , N-Diarylalkenyl-piperidinecarboxylic acid derivatives
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796350
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