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Antiobesity designed multiple ligands: Synthesis of pyrazole fatty acid amides and evaluation as hypophagic agents

Autor(es) y otros:
Alvarado Narváez, Mario; Goya Laza, Pilar; Macías González, Manuel; Pavón, Francisco Javier; Serrano, Antonia; Jagerovic, Nadine; Elguero Bertolini, José; Gutiérrez Rodríguez, ÁngelAutoridad Uniovi; García-Granda, SantiagoAutoridad Uniovi; Suardíaz, Margarita; Rodríguez de Fonseca, Fernando
Palabra(s) clave:

Pyrazole; Oleylamide; Pparα; Dmls

Fecha de publicación:
2008
Versión del editor:
http://dx.doi.org/10.1016/j.bmc.2008.10.023
Citación:
Bioorganic & Medicinal Chemistry, 16(23), P. 10098-10105 (2008); doi:10.1016/j.bmc.2008.10.023
Descripción física:
p. 10098-10105
Resumen:

Searching for new antiobesity agents, a new series of fatty acid amide derivatives of 1,5-diarylpyrazole have been synthesized as dual peroxisome proliferator activated receptor alpha (PPARα)/cannabinoid receptor ligands. The compounds have been evaluated in vivo and in vitro as PPARα activators and as cannabinoids in two tests of the mouse tetrad. In vivo, food intake studies have been performed with all the compounds. No significant cannabinoid activity has been found but some compounds behaved as potent PPARα activators. Several compounds showed anorexigenic properties reducing food intake in rats.

Searching for new antiobesity agents, a new series of fatty acid amide derivatives of 1,5-diarylpyrazole have been synthesized as dual peroxisome proliferator activated receptor alpha (PPARα)/cannabinoid receptor ligands. The compounds have been evaluated in vivo and in vitro as PPARα activators and as cannabinoids in two tests of the mouse tetrad. In vivo, food intake studies have been performed with all the compounds. No significant cannabinoid activity has been found but some compounds behaved as potent PPARα activators. Several compounds showed anorexigenic properties reducing food intake in rats.

URI:
http://hdl.handle.net/10651/10148
ISSN:
0968-0896
Identificador local:

450

DOI:
10.1016/j.bmc.2008.10.023
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