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

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Faucher N, Martres P, Laroze A, Pineau O, Potvain F, Grillot D

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. Epub 2007 Nov 21.

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18060776 [ View in PubMed

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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.

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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
GW-590735	Peroxisome proliferator-activated receptor alpha	EC 50 (nM)	4	N/A	N/A	Details