A new synthesis method and GABA transporters inhibitory activities of Tiagabine and its analogues

Jian Ge Zhang*, Chang Sheng Jiang, Jian Bin Zheng, Ren Wen, Guo Qiang Lin

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

1 Scopus citations

Abstract

A new synthetic method and GABA transporter inhibitory activities of Tiagabine and its analogues are described. The key intermediates 4-tosyl-1,1-diaryl/heteroaryl-1-butene 10a-10e were synthesized by Wittig reaction, and followed by W-alkylation with (R)-3-piperidinecarboxylate. The resulting N-diheterocyclylalkenylpiperidine-3-carboxylic acid ester 11a-11e were saponified and then acidified to-get the target compounds 1a-1e. The preliminary bioassays show that compounds 1a-1e exhibited excellent inhibition of [3H]-GABA uptake in vitro of culture cells.

Original languageEnglish (US)
Pages (from-to)351-355
Number of pages5
JournalChemical Research in Chinese Universities
Volume22
Issue number3
DOIs
StatePublished - May 2006

Keywords

  • Analogue
  • GABA transporter inhibitor
  • Synthesis
  • Tiagabine

ASJC Scopus subject areas

  • Chemistry(all)

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