Design, synthesis and evaluation of trifluoromethane sulfonamide derivatives as new potent and selective peroxisome proliferator-activated receptor alpha agonists.
Starting from the structure of 5, a two-step strategy was applied to identify a new generation of trifluoromethane sulfonamides as potent PPARalpha agonists. Synthesis, in vitro and in vivo evaluation of the most potent compound are reported.
Department of Medicinal Chemistry, Laboratoire GlaxoSmithKline, Centre de Recherches, 25-27 avenue du Québec, 91951 Les Ulis, France. nicolas. faucher@gsk.com
Nicolas
N
Faucher
Paul
P
Martres
Alain
A
Laroze
Olivier
O
Pineau
Florent
F
Potvain
Didier
D
Grillot
D000818:Animals; D002460:Cell Line; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006801:Humans; D051379:Mice; D047493:PPAR alpha / Q000819:agonists*; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
D047493:PPAR alpha; D013449:Sulfonamides