title: Novel antiobesity agents: synthesis and pharmacological evaluation of analogues of Rimonabant and of LH21.
abstract: Searching 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.
authors: Instituto de Química Médica, CSIC, Juan de Cierva 3, E-28006 Madrid, Spain.
authors: Mario
authors: M
authors: Alvarado
authors: Juan
authors: J
authors: Decara
authors: María Jesús
authors: MJ
authors: Luque
authors: Laura
authors: L
authors: Hernandez-Folgado
authors: María
authors: M
authors: Gómez-Cañas
authors: María
authors: M
authors: Gómez-Ruiz
authors: Javier
authors: J
authors: Fernández-Ruiz
authors: José
authors: J
authors: Elguero
authors: Nadine
authors: N
authors: Jagerovic
authors: Antonia
authors: A
authors: Serrano
authors: Pilar
authors: P
authors: Goya
authors: Fernando Rodríguez
authors: FR
authors: de Fonseca
mesh_terms: D000818:Animals; D019440:Anti-Obesity Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002186:Cannabinoids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D004435:Eating / Q000187:drug effects*; D006801:Humans; D008297:Male; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D043884:Receptor, Cannabinoid, CB1 / Q000378:metabolism; D043885:Receptor, Cannabinoid, CB2 / Q000378:metabolism; D000077285:Rimonabant
chemical_list: D019440:Anti-Obesity Agents; D002186:Cannabinoids; D010880:Piperidines; D011720:Pyrazoles; D043884:Receptor, Cannabinoid, CB1; D043885:Receptor, Cannabinoid, CB2; D000077285:Rimonabant