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Eur J Med Chem. 2014 Mar 21;75:159-68. doi: 10.1016/j.ejmech.2014.01.055. Epub 2014 Jan 28.

New 1-arylindoles based serotonin 5-HT7 antagonists. Synthesis and binding evaluation studies.

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  • 1Institut de Chimie et Biochimie Moléculaires et Supramoléculaires, UMR CNRS 5246, Université de Lyon, Université Claude Bernard - Lyon 1, Bâtiment Curien, 43 Bd du 11 Novembre 1918, F-69622 Villeurbanne, France.
  • 2Department of Medicinal Chemistry, Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Street, 31-343 Kraków, Poland.
  • 3Department of Medicinal Chemistry, Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Street, 31-343 Kraków, Poland. Electronic address: bojarski@if-pan.krakow.pol.
  • 4Institut de Chimie et Biochimie Moléculaires et Supramoléculaires, UMR CNRS 5246, Université de Lyon, Université Claude Bernard - Lyon 1, Bâtiment Curien, 43 Bd du 11 Novembre 1918, F-69622 Villeurbanne, France. Electronic address: benoit.joseph@univ-lyon1.fr.

Abstract

Based on 5-HT1A and 5-HT7 ligand MR25003 scaffold, a new series of 1-aryl indole analogues were prepared and evaluated against 5-HT7 receptors. Modulations of aryl moieties provided a large number of new indolic derivatives. Most of compounds tested have displayed 5-HT7 affinity in the nanomolar range. Among them, 1-(naphthyl)indole derivative 3p (Ki (5-HT7) = 4.5 nM) showed also a good selectivity over 5-HT1A, 5-HT2A and 5-HT6 receptors. This compound was pharmacology characterized as an antagonist.

Copyright © 2014 Elsevier Masson SAS. All rights reserved.

KEYWORDS:

5-HT(1A); 5-HT(7); Antagonist; Indole; Serotonin

PMID:
24531229
[PubMed - indexed for MEDLINE]
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