Published in
Elsevier, Bioorganic and Medicinal Chemistry, 7(21), p. 1708-1716
DOI: 10.1016/j.bmc.2013.01.055
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Novel antiobesity agents: Synthesis and pharmacological evaluation of analogues of Rimonabant and of LH21
,
María Gómez-Ruiz,
Fernando Rodríguez de Fonseca,
Javier Fernández-Ruiz,
José Elguero,
Nadine Jagerovic ,
Pilar Goya,
Antonia Serrano
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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.