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.
Faucher
Nicolas
N
Department of Medicinal Chemistry, Laboratoire GlaxoSmithKline, Centre de Recherches, 25-27 avenue du Québec, 91951 Les Ulis, France. nicolas. faucher@gsk.com
Martres
Paul
P
Laroze
Alain
A
Pineau
Olivier
O
Potvain
Florent
F
Grillot
Didier
D
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