Design, synthesis and evaluation of trifluoromethane sulfonamide derivatives as new potent and selective peroxisome proliferator-activated receptor alpha agonists

Nicolas Faucher; Paul Martres; Alain Laroze; Olivier Pineau; Florent Potvain; Didier Grillot

doi:10.1016/j.bmcl.2007.11.053

Design, synthesis and evaluation of trifluoromethane sulfonamide derivatives as new potent and selective peroxisome proliferator-activated receptor alpha agonists

Bioorg Med Chem Lett. 2008 Jan 15;18(2):710-5. doi: 10.1016/j.bmcl.2007.11.053. Epub 2007 Nov 21.

Authors

Nicolas Faucher¹, Paul Martres, Alain Laroze, Olivier Pineau, Florent Potvain, Didier Grillot

Affiliation

¹ Department of Medicinal Chemistry, Laboratoire GlaxoSmithKline, Centre de Recherches, 25-27 avenue du Québec, 91951 Les Ulis, France. nicolas. faucher@gsk.com

PMID: 18060776
DOI: 10.1016/j.bmcl.2007.11.053

Abstract

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.

MeSH terms

Animals
Cell Line
Drug Design
Drug Evaluation, Preclinical
Humans
Mice
PPAR alpha / agonists*
Sulfonamides / chemical synthesis
Sulfonamides / chemistry*
Sulfonamides / pharmacology*

Substances

PPAR alpha
Sulfonamides