New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and Pharmacological in Vitro and in Vivo Evaluations

Aline Moulin; Luc Demange; Joanne Ryan; Delphine Mousseaux; Pierre Sanchez; Gilbert Bergé; Didier Gagne; Daniel Perissoud; Vittorio Locatelli; Antonio Torsello; Jean-Claude Galleyrand; Jean Martinez; Jean-Alain Fehrentz

doi:10.1021/jm701292s

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New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and Pharmacological in Vitro and in Vivo Evaluations

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New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and Pharmacological in Vitro and in Vivo Evaluations

Aline Moulin, Luc Demange, Joanne Ryan, Delphine Mousseaux, Pierre Sanchez, Gilbert Bergé, Didier Gagne, Daniel Perissoud, Vittorio Locatelli, Antonio Torsello, …

Journal of Medicinal Chemistry, Vol.51, pp.689-693

2008

DOI: https://doi.org/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 R-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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Title: New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and Pharmacological in Vitro and in Vivo Evaluations
Creators - without role: Aline Moulin - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Luc Demange - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Joanne Ryan - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Delphine Mousseaux - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Pierre Sanchez - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Gilbert Bergé - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Didier Gagne - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Daniel Perissoud - Zentaris GmbH
Vittorio Locatelli - University of Milano-Bicocca
Antonio Torsello - Institut des Biomolécules Max Mousseron
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: Journal of Medicinal Chemistry, Vol.51, pp.689-693
Identifiers: 9944150409311
Academic Unit: Institut des Biomolécules Max Mousseron - IBMM
Language: English
Resource Type: Journal article
Local Fields: hal-00341585