Literature DB >> 19443217

Synthesis and biological evaluation of novel gamma-carboline analogues of Dimebon as potent 5-HT6 receptor antagonists.

Alexandre V Ivachtchenko1, Eugene B Frolov, Oleg D Mitkin, Volodymyr M Kysil, Alexander V Khvat, Ilya M Okun, Sergey E Tkachenko.   

Abstract

Synthesis, biological evaluation and structure-activity relationships for a series of novel gamma-carboline analogues of Dimebon are described. Among the studied compounds, gamma-carbolines 3{8} and 3{14} have been identified as potent small molecule antagonists of histamine H(1) (IC(50)=0.1 microM) and serotonin 5-HT(6) (IC(50)=0.37 microM) receptors, respectively.

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Year:  2009        PMID: 19443217     DOI: 10.1016/j.bmcl.2009.04.128

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


  6 in total

1.  Ruthenium-catalyzed γ-carbolinium ion formation from aryl azides; synthesis of dimebolin.

Authors:  Huijun Dong; Regina T Latka; Tom G Driver
Journal:  Org Lett       Date:  2011-04-25       Impact factor: 6.005

2.  Identification, Structure-Activity Relationship, and Biological Characterization of 2,3,4,5-Tetrahydro-1H-pyrido[4,3-b]indoles as a Novel Class of CFTR Potentiators.

Authors:  Nicoletta Brindani; Ambra Gianotti; Simone Giovani; Francesca Giacomina; Paolo Di Fruscia; Federico Sorana; Sine Mandrup Bertozzi; Giuliana Ottonello; Luca Goldoni; Ilaria Penna; Debora Russo; Maria Summa; Rosalia Bertorelli; Loretta Ferrera; Emanuela Pesce; Elvira Sondo; Luis J V Galietta; Tiziano Bandiera; Nicoletta Pedemonte; Fabio Bertozzi
Journal:  J Med Chem       Date:  2020-09-18       Impact factor: 7.446

3.  The gramine route to pyrido[4,3-b]indol-3-ones - identification of a new cytotoxic lead.

Authors:  Uwe Wollein; Franz Bracher
Journal:  Sci Pharm       Date:  2010-12-18

4.  Bioisosteric matrices for ligands of serotonin receptors.

Authors:  Dawid Warszycki; Stefan Mordalski; Jakub Staroń; Andrzej J Bojarski
Journal:  ChemMedChem       Date:  2015-03-13       Impact factor: 3.466

5.  Stereodivergent assembly of tetrahydro-γ-carbolines via synergistic catalytic asymmetric cascade reaction.

Authors:  Shi-Ming Xu; Liang Wei; Chong Shen; Lu Xiao; Hai-Yan Tao; Chun-Jiang Wang
Journal:  Nat Commun       Date:  2019-12-05       Impact factor: 14.919

6.  Multi-Target-Directed Ligands and other Therapeutic Strategies in the Search of a Real Solution for Alzheimer's Disease.

Authors:  Angel Agis-Torres; Monica Sölhuber; Maria Fernandez; J M Sanchez-Montero
Journal:  Curr Neuropharmacol       Date:  2014-01       Impact factor: 7.363

  6 in total

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