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

Aline Moulin; L. Demange; J. Ryan; Celine M'Kadmi; Jean-Claude Galleyrand; Jean Martinez; Jean-Alain Fehrentz

doi:10.1016/j.bmcl.2007.10.113

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

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

Aline Moulin, L. Demange, J. Ryan, Celine M'Kadmi, Jean-Claude Galleyrand, Jean Martinez and Jean-Alain Fehrentz

Bioorganic and Medicinal Chemistry Letters, Vol.18(1), pp.164-168

2008

DOI: https://doi.org/10.1016/j.bmcl.2007.10.113

Abstract

bond

agonist

antagonist

ghrelin

growth-hormone secretagogue

peptide

ghs-rla

4-triazole

trisubstituted 1

4-triazoles

ghrelin receptor ligands

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. (C) 2007 Elsevier Ltd. All rights reserved.

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Title: Trisubstituted 1,2,4-triazoles as ligands for the ghrelin receptor: On the significance of the orientation and substitution at position 3
Creators - without role: Aline Moulin - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
L. Demange - Institut des Biomolécules Max Mousseron
J. Ryan - Institut des Biomolécules Max Mousseron
Celine M'Kadmi - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Jean-Claude Galleyrand - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Jean Martinez - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Jean-Alain Fehrentz - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Publication Details: Bioorganic and Medicinal Chemistry Letters, Vol.18(1), pp.164-168
Identifiers: 9947116509311
Academic Unit: Institut des Biomolécules Max Mousseron - IBMM
Language: English
Resource Type: Journal article
Local Fields: hal-00420056