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

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Alvarado M, Decara J, Luque MJ, Hernandez-Folgado L, Gomez-Canas M, Gomez-Ruiz M, Fernandez-Ruiz J, Elguero J, Jagerovic N, Serrano A, Goya P, de Fonseca FR

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

Bioorg Med Chem. 2013 Apr 1;21(7):1708-16. doi: 10.1016/j.bmc.2013.01.055. Epub 2013 Feb 4.

PubMed ID

23434135 [ View in PubMed

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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 alpha,beta-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.

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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Rimonabant	Cannabinoid receptor 1	Ki (nM)	7.3	N/A	N/A	Details