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

Aline Moulin; Luc Demange; Joanne Ryan; Céline M'Kadmi; Jean-Claude Galleyrand; Jean Martinez; Jean-Alain Fehrentz

doi:10.1016/j.bmcl.2007.10.113

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

Bioorg Med Chem Lett. 2008 Jan 1;18(1):164-8. doi: 10.1016/j.bmcl.2007.10.113. Epub 2007 Nov 4.

Authors

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

Affiliation

¹ Institut des Biomolécules Max Mousseron, UMR 5247, CNRS-Université Montpellier I, BP 14491, Faculté de Pharmacie, 15 avenue Charles Flahault, 34093 Montpellier Cedex 5, France.

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

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.

MeSH terms

Ligands
Receptors, Ghrelin / agonists
Receptors, Ghrelin / antagonists & inhibitors
Receptors, Ghrelin / chemistry*
Receptors, Ghrelin / metabolism
Structure-Activity Relationship
Triazoles / chemical synthesis
Triazoles / chemistry*
Triazoles / metabolism
Triazoles / pharmacology

Substances

Ligands
Receptors, Ghrelin
Triazoles