Identification and synthesis of a novel selective partial PPARδ agonist with full efficacy on lipid metabolism in vitro and in vivo

…, L Jeppesen, JP Mogensen, I Pettersson…

Index: Sauerberg, Per; Olsen, Grith S.; Jeppesen, Lone; Mogensen, John P.; Pettersson, Ingrid; Jeppesen, Claus B.; Daugaard, Jens R.; Galsgaard, Elisabeth D.; Ynddal, Lars; Fleckner, Jan; Panajotova, Vladimira; Polivka, Zdenek; Pihera, Pavel; Havranek, Miroslav; Wulff, Erik M. Journal of Medicinal Chemistry, 2007 , vol. 50, # 7 p. 1495 - 1503

Full Text: HTML

Citation Number: 30

Abstract

The aim was to identify a novel selective PPARδ agonist with full efficacy on free fatty acid (FFA) oxidation in vitro and plasma lipid correction in vivo. Using the triple PPARα, γ, δ agonist 1 as the structural starting point, we wanted to investigate the possibility of obtaining selective PPARδ agonists by modifying only the acidic part of 1, while holding the lipophilic half of the molecule constant. The structure-activity relationship was guided by in vitro ...