Literature DB >> 18023181

Trisubstituted 1,2,4-triazoles as ligands for the ghrelin receptor: on the significance of the orientation and substitution at position 3.

Aline Moulin1, Luc Demange, Joanne Ryan, Céline M'Kadmi, Jean-Claude Galleyrand, Jean Martinez, Jean-Alain Fehrentz.   

Abstract

The synthesis and structure-activity relationships concerning 3,4,5-trisubstituted 1,2,4-triazoles as ghrelin receptor ligands are described. The importance of the starting aminoacid material as well as its configuration was explored and the (D) Trp residue was found to lead to the best agonist or antagonist compounds.

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Year:  2007        PMID： 18023181     DOI： 10.1016/j.bmcl.2007.10.113

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


  5 in total

Review 1.  Constitutive activation of G protein-coupled receptors and diseases: insights into mechanisms of activation and therapeutics.

Authors:  Ya-Xiong Tao
Journal:  Pharmacol Ther       Date:  2008-08-09       Impact factor: 12.310

2.  Detection of a target protein (GroEl2) in Mycobacterium tuberculosis using a derivative of 1,2,4-triazolethiols.

Authors:  Sampa Sarkar; Sagar Swami; Sarvesh Kumar Soni; Jessica K Holien; Arshad Khan; Arvind M Korwar; Anjali P Likhite; Ramesh A Joshi; Rohini R Joshi; Dhiman Sarkar
Journal:  Mol Divers       Date:  2021-11-25       Impact factor: 3.364

3.  Conformationally homogeneous heterocyclic pseudotetrapeptides as three-dimensional scaffolds for rational drug design: receptor-selective somatostatin analogues.

Authors:  John M Beierle; W Seth Horne; Jan H van Maarseveen; Beatrice Waser; Jean Claude Reubi; M Reza Ghadiri
Journal:  Angew Chem Int Ed Engl       Date:  2009       Impact factor: 15.336

4.  Rapid sensing of circulating ghrelin by hypothalamic appetite-modifying neurons.

Authors:  Marie Schaeffer; Fanny Langlet; Chrystel Lafont; François Molino; David J Hodson; Thomas Roux; Laurent Lamarque; Pascal Verdié; Emmanuel Bourrier; Bénédicte Dehouck; Jean-Louis Banères; Jean Martinez; Pierre-François Méry; Jacky Marie; Eric Trinquet; Jean-Alain Fehrentz; Vincent Prévot; Patrice Mollard
Journal:  Proc Natl Acad Sci U S A       Date:  2013-01-07       Impact factor: 11.205

5.  Recent advances in potential clinical application of ghrelin in obesity.

Authors:  Christine Delporte
Journal:  J Obes       Date:  2012-02-20
  5 in total

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