Novel antiobesity agents: Synthesis and pharmacological evaluation of analogues of Rimonabant and of LH21
作者: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
DOI:10.1016/j.bmc.2013.01.055
日期:2013.4
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
为了寻找新型的抗肥胖药,已经制备了一系列大麻素LH21和利莫那班-脂肪酸酰胺类似物。吡唑2a – 2c的合成是通过两步简单的方法,通过α,β-不饱和酮实现的。通过在温和条件下进行的一锅法操作,从酯7a - 7c中以高收率获得了羧酰胺8a - 8h。已经在体内评估了新化合物作为厌食药的作用。他们中的一些人表现出令人感兴趣的特性,其通过不涉及内源性大麻素系统的机制减少了大鼠的食物摄入。