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Title

Novel antiobesity agents: Synthesis and pharmacological evaluation of analogues of Rimonabant and of LH21

AuthorsAlvarado, Mario ; Decara, Juan; Luque, María Jesús; Hernández-Folgado, Laura ; Gómez-Cañas, María; Gómez-Ruiz, María; Fernández-Ruiz, Javier; Elguero, José ; Jagerovic, Nadine ; Serrano, Antonia; Goya, Pilar ; De Fonseca, Fernando R.
KeywordsRimonabant
LH21
Pyrazole alkylamides
Triazole alkylamides
Cannabinoid
Issue Date2013
PublisherPergamon Press
CitationBioorganic and Medicinal Chemistry 21: 1708- 1716 (2013)
AbstractSearching for novel antiobesity agents, a series of cannabinoid LH21 and of Rimonabant-fatty acid amide analogues have been prepared. Synthesis of pyrazoles 2a-2c was achieved by a two steps simple methodology via α,β-unsaturated ketones. Carboxamides 8a-8h were obtained in good yields from esters 7a-7c by a one-pot procedure which takes place under mild conditions. New compounds have been evaluated in vivo as anorectic agents. Some of them showed interesting properties reducing food intake in rats by a mechanism which does not involve the endocannabinoid system.
URIhttp://hdl.handle.net/10261/101434
DOI10.1016/j.bmc.2013.01.055
Identifiersdoi: 10.1016/j.bmc.2013.01.055
issn: 0968-0896
e-issn: 1464-3391
Appears in Collections:(IQM) Artículos
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