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.

Moulin, A., Demange, L., Ryan, J., Mousseaux, D., Sanchez, P., Bergé, G., et al. (2008). New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and pharmacological in vitro and in vivo evaluations. JOURNAL OF MEDICINAL CHEMISTRY, 51(3), 689-693 [10.1021/jm701292s].

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

LOCATELLI, VITTORIO;TORSELLO, ANTONIO BIAGIO;
2008

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.
Articolo in rivista - Articolo scientifico
GHS, GH
English
689
693
5
Moulin, A., Demange, L., Ryan, J., Mousseaux, D., Sanchez, P., Bergé, G., et al. (2008). New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and pharmacological in vitro and in vivo evaluations. JOURNAL OF MEDICINAL CHEMISTRY, 51(3), 689-693 [10.1021/jm701292s].
Moulin, A; Demange, L; Ryan, J; Mousseaux, D; Sanchez, P; Bergé, G; Gagne, D; Perrissoud, D; Locatelli, V; Torsello, A; Galleyrand, J; Fehrentz, J; Martinez, J
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10281/6107
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