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

Jianbin Zheng, Ren Wen*, Xiaomin Luo, Guoqiang Lin, Jiange Zhang, Linfeng Xu, Lihe Guo, Hualiang Jiang

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

16 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)225-227
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number1
DOIs
StatePublished - Jan 1 2006

Keywords

  • Antiepileptic
  • GABA uptake inhibitors
  • GAT1
  • N-Diarylalkenyl- piperidinecarboxylic acid derivatives

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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