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Novel oxazolidinone based PPAR agonists: molecular modeling, synthesis and biological evaluation

AutorFresno, Nieves ; Macías-González, Manuel; Torres-Zaguirre, A.; Romero-Cuevas, Miguel; Sanz-Camacho, P.; Elguero, José ; Pavón, J.; Rodríguez De Fonseca, F.; Goya, Pilar ; Pérez-Fernández, Ruth
Palabras claveOxazolidinone
PPAR agonists
Molecular modeling
Metabolic syndrome
Diabetes
Fecha de publicación27-ago-2015
EditorAmerican Chemical Society
CitaciónJ. Med. Chem. 58 (16) 6639–6652 (2015)
ResumenA series of new peroxisome proliferator activated receptors (PPARs) chiral ligands have been designed following the accepted three-module structure comprising a polar head, linker, and hydrophobic tail. The majority of the ligands incorporate the oxazolidinone moiety as a novel polar head, and the nature of the hydrophobic tail has also been varied. Docking studies using the crystal structure of an agonist bound to the ligand binding domain of the PPARα receptor have been performed as a tool for their design. Suitable synthetic procedures have been developed, and compounds with different stereochemistries have been prepared. Evaluation of basal and ligand-induced activity proved that several compounds showed agonist activity at the PPARα receptor, thus validating the oxazolidinone template for PPAR activity. In addition, two compounds, 2 and 4, showed dual PPARα/PPARγ agonism and interesting food intake reduction in rats.
Descripción49 p.-7 fig.-2 tab.
Versión del editorhttp://dx.doi.org/ 10.1021/acs.jmedchem.5b00849
URIhttp://hdl.handle.net/10261/121997
DOI10.1021/acs.jmedchem.5b00849
ISSN0022-2623
E-ISSN1520-4804
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