Studies towards the conception of new selective PPARbeta/delta ligands.
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.
Basséne
Carine Ekambomé
CE
Institut de Chimie Organique et Analytique (ICOA), UMR-CNRS 6005, FR CNRS 2708, Université d'Orléans, France.
Suzenet
Franck
F
Hennuyer
Nathalie
N
Staels
Bart
B
Caignard
Daniel-Henri
DH
Dacquet
Catherine
C
Renard
Pierre
P
Guillaumet
Gérald
G
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
D008024:Ligands; D047494:PPAR delta; D048068:PPAR-beta