Novel antiobesity agents: synthesis and pharmacological evaluation of analogues of Rimonabant and of LH21.

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. Copyright © 2013 Elsevier Ltd. All rights reserved.

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Mario Alvarado, Juan Decara, María Jesús Luque, Laura Hernandez-Folgado, María Gómez-Cañas, María Gómez-Ruiz, Javier Fernández-Ruiz, José Elguero, Nadine Jagerovic, Antonia Serrano, Pilar Goya, Fernando Rodríguez de Fonseca. Novel antiobesity agents: synthesis and pharmacological evaluation of analogues of Rimonabant and of LH21. Bioorganic & medicinal chemistry. 2013 Apr 1;21(7):1708-16

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PMID: 23434135

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