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Discovery of Potent Dual PPAR alpha Agonists/CB1 Ligands

AuthorsPérez-Fernández, Ruth ; Fresno, Nieves ; Macías-González, Manuel; Elguero, José ; Decara, Juan; Girón, Rocío; Rodríguez-Álvarez, Ana; Martín, María Isabel; Rodríguez de Fonseca, Fernando; Goya, Pilar
KeywordsDual ligands
Issue Date2011
PublisherAmerican Chemical Society
CitationMedicinal Chemistry Letters 2 : 793–797 (2011)
AbstractABSTRACT: This letter describes the synthesis and in vitro and in vivo evaluation of dual ligands targeting the cannabinoid and peroxisome proliferator-activated receptors (PPAR). These com- pounds were obtained from fusing the pharmacophores of fibrates and the diarylpyrazole rimonabant, a cannabinoid receptor an- tagonist. They are the first examples of dual compounds with nanomolar affinity for both PPARα and cannabinoid receptors. Besides, lead compound 2 proved to be CB1 selective. Unexpect- edly, the phenol intermediates tested were equipotent (compound 1 as compared to 2) or even more potent (compound 3 as compared with 4). This discovery opens the way to design new dual ligands.
Publisher version (URL)http://dx.doi.org/10.1021/ml200091q
Appears in Collections:(IQM) Artículos
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