Literature DB >> 16246548

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

Jianbin Zheng1, Ren Wen, Xiaomin Luo, Guoqiang Lin, Jiange Zhang, Linfeng Xu, Lihe Guo, Hualiang Jiang.   

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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Year:  2005        PMID： 16246548     DOI： 10.1016/j.bmcl.2005.09.004

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

1.  Development of Positron Emission Tomography Radiotracers for the GABA Transporter 1.

Authors:  Alexandra R Sowa; Allen F Brooks; Xia Shao; Bradford D Henderson; Philip Sherman; Janna Arteaga; Jenelle Stauff; Adam C Lee; Robert A Koeppe; Peter J H Scott; Michael R Kilbourn
Journal:  ACS Chem Neurosci       Date:  2018-05-24       Impact factor: 4.418

2.  Classification of High-Activity Tiagabine Analogs by Binary QSAR Modeling.

Authors:  Andreas Jurik; Regina Reicherstorfer; Barbara Zdrazil; Gerhard F Ecker
Journal:  Mol Inform       Date:  2013-05-15       Impact factor: 4.050

3.  Development of MLR and SVM Aided QSAR Models to Identify Common SAR of GABA Uptake Herbal Inhibitors used in the Treatment of Schizophrenia.

Authors:  Sahila Mohammed Marunnan; Babitha Pallikkara Pulikkal; Anitha Jabamalairaj; Srinivas Bandaru; Mukesh Yadav; Anuraj Nayarisseri; Victor Arokia Doss
Journal:  Curr Neuropharmacol       Date:  2017-11-14       Impact factor: 7.363

4.  GRID-independent molecular descriptor analysis and molecular docking studies to mimic the binding hypothesis of γ-aminobutyric acid transporter 1 (GAT1) inhibitors.

Authors:  Sadia Zafar; Ishrat Jabeen
Journal:  PeerJ       Date:  2019-01-31       Impact factor: 2.984

5.  Molecular docking based screening of GABA (A) receptor inhibitors from plant derivatives.

Authors:  Mohammed Marunnan Sahila; Pallikkara Pulikkal Babitha; Srinivas Bandaru; Anuraj Nayarisseri; Victor Arokia Doss
Journal:  Bioinformation       Date:  2015-06-30

Review 6.  Structure, Function, and Modulation of γ-Aminobutyric Acid Transporter 1 (GAT1) in Neurological Disorders: A Pharmacoinformatic Prospective.

Authors:  Sadia Zafar; Ishrat Jabeen
Journal:  Front Chem       Date:  2018-09-11       Impact factor: 5.221
  6 in total

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