Substituted 2-[(4-aminomethyl) phenoxy]-2-methylpropionic acid PPARα agonists. 1. Discovery of a novel series of potent HDLc raising agents

ML Sierra, V Beneton, AB Boullay, T Boyer…

Index: Sierra, Michael L.; Beneton, Veronique; Boullay, Anne-Benedict; Boyer, Thierry; Brewster, Andrew G.; Donche, Frederic; Forest, Marie-Claire; Fouchet, Marie-Helene; Gellibert, Francoise J.; Grillot, Didier A.; Lambert, Millard H.; Laroze, Alain; Le Grumelec, Christelle; Linget, Jean Michel; Montana, Valerie G.; Nguyen, Van-Loc; Nicodeme, Edwige; Patel, Vipul; Penfornis, Annie; Pineau, Olivier; Pohin, Danig; Potvain, Florent; Poulain, Geraldine; Ruault, Cecile Bertho; Saunders, Michael; Toum, Jerome; Xu, H. Eric; Xu, Robert X.; Pianetti, Pascal M. Journal of Medicinal Chemistry, 2007 , vol. 50, # 4 p. 685 - 695

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Citation Number: 89

Abstract

The peroxisome proliferator activated receptors PPARα, PPARγ, and PPARδ are ligand- activated transcription factors that play a key role in lipid homeostasis. The fibrates raise circulating levels of high-density lipoprotein cholesterol and lower levels of triglycerides in part through their activity as PPARα agonists; however, the low potency and restricted selectivity of the fibrates may limit their efficacy, and it would be desirable to develop more ...