2. Academic Validation
  3. New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and pharmacological in vitro and in vivo evaluations

New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and pharmacological in vitro and in vivo evaluations

  • J Med Chem. 2008 Feb 14;51(3):689-93. doi: 10.1021/jm701292s.
Aline Moulin 1,  Luc Demange,  Joanne Ryan,  Delphine Mousseaux,  Pierre Sanchez,  Gilbert Bergé,  Didier Gagne,  Daniel Perrissoud,  Vittorio Locatelli,  Antonio Torsello,  Jean-Claude Galleyrand,  Jean-Alain Fehrentz,  Jean Martinez
Affiliations

Affiliation

  • 1 Institut des Biomolécules Max Mousseron, UMR 5247, CNRS, Universités Montpellier 1, Montpellier 2, Montpellier Cedex 5, France.
PMID: 18193826 DOI: 10.1021/jm701292s
Abstract

Ghrelin receptor ligands based on trisubstituted 1,2,4-triazole structure were synthesized and evaluated for their in vitro binding and biological activity. In this study, we explored the replacement of the alpha-aminoisobutyryl moiety by aromatic or heteroaromatic groups. Compounds 5 and 34 acted as potent in vivo antagonists of hexarelin-stimulated food intake. These two compounds did not stimulate growth hormone secretion in rodents and did not antagonize growth hormone secretion induced by hexarelin.

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