2024-03-28T16:41:25Zhttp://digital.csic.es/dspace-oai/requestoai:digital.csic.es:10261/438372022-11-08T10:43:16Zcom_10261_81com_10261_5col_10261_334
DIGITAL.CSIC
author
Pérez-Fernández, Ruth
author
Fresno, Nieves
author
Macías-González, Manuel
author
Elguero, José
author
Decara, Juan
author
Girón, Rocío
author
Rodríguez-Álvarez, Ana
author
Martín, María Isabel
author
Rodríguez de Fonseca, Fernando
author
Goya, Pilar
2011-12-30T09:52:23Z
2011-12-30T09:52:23Z
2011
Medicinal Chemistry Letters 2 : 793–797 (2011)
1948-5875
http://hdl.handle.net/10261/43837
10.1021/ml200091q
24936232
ABSTRACT: 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.
eng
closedAccess
Dual ligands
PPARα
cannabinoids
rimonabant
fibrates
neuroprotective
Discovery of Potent Dual PPAR alpha Agonists/CB1 Ligands
artículo
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