title: Studies towards the conception of new selective PPARbeta/delta ligands.
abstract: In order to define new PPARbeta/delta ligands, SAR study on the selective PPARbeta/delta activator L-165,041 led to the identification of one key functional group for selective PPARbeta/delta activation. Furthermore, taking advantage of SAR studies done elsewhere on the most selective PPARbeta/delta ligand GW501516, the conception of new ligands showing good affinity for PPARbeta/delta is reported. Finally, synthesis and biological evaluation of pyridine analogues have shown the benefical effect of the pyridine ring on the PPARbeta/delta subtype selectivity.
authors.affiliation: Institut de Chimie Organique et Analytique (ICOA), UMR-CNRS 6005, FR CNRS 2708, Université d'Orléans, France.
authors.forename: Carine Ekambomé
authors.initials: CE
authors.lastname: Basséne
authors.forename: Franck
authors.initials: F
authors.lastname: Suzenet
authors.forename: Nathalie
authors.initials: N
authors.lastname: Hennuyer
authors.forename: Bart
authors.initials: B
authors.lastname: Staels
authors.forename: Daniel-Henri
authors.initials: DH
authors.lastname: Caignard
authors.forename: Catherine
authors.initials: C
authors.lastname: Dacquet
authors.forename: Pierre
authors.initials: P
authors.lastname: Renard
authors.forename: Gérald
authors.initials: G
authors.lastname: Guillaumet
mesh_terms: D000818:Animals; D019556:COS Cells; D002522:Chlorocebus aethiops; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D047494:PPAR delta / Q000737:chemistry* / Q000378:metabolism*; D048068:PPAR-beta / Q000737:chemistry* / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D008024:Ligands; D047494:PPAR delta; D048068:PPAR-beta