New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and pharmacological in vitro and in vivo evaluations
| Autor: | Gilbert Bergé, Jean Martinez, Jean-Alain Fehrentz, Delphine Mousseaux, Daniel Perrissoud, Luc Demange, Aline Moulin, Vittorio Locatelli, Joanne Ryan, Jean Claude Galleyrand, Pierre Sanchez, Didier Gagne, Antonio Torsello |
|---|---|
| Přispěvatelé: | Institut des Biomolécules Max Mousseron [Pôle Chimie Balard] (IBMM), Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC)-Université de Montpellier (UM)-Ecole Nationale Supérieure de Chimie de Montpellier (ENSCM), Zentaris GmbH, Università degli Studi di Milano-Bicocca [Milano] (UNIMIB), 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 |
| Rok vydání: | 2008 |
| Předmět: |
Swine
01 natural sciences Chemical synthesis GHS GH 03 medical and health sciences Eating Radioligand Assay Structure-Activity Relationship In vivo Drug Discovery Moiety Animals Humans Receptor Receptors Ghrelin BIO/14 - FARMACOLOGIA 030304 developmental biology 0303 health sciences 010405 organic chemistry Chemistry [CHIM.ORGA]Chemical Sciences/Organic chemistry Biological activity Stereoisomerism Triazoles Growth hormone secretion In vitro 3. Good health 0104 chemical sciences Rats Biochemistry Growth Hormone Pyrazines Picolines Molecular Medicine LLC-PK1 Cells Ghrelin Anti-Obesity Agents Oligopeptides |
| Zdroj: | Journal of Medicinal Chemistry Journal of Medicinal Chemistry, American Chemical Society, 2008, 51, pp.689-693. ⟨10.1021/jm701292s⟩ |
| ISSN: | 0022-2623 1520-4804 |
| DOI: | 10.1021/jm701292s⟩ |
| Popis: | International audience; 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|