Glycine amides as PPARα agonists

• Published in: Bioorganic & medicinal chemistry letters Vol. 20; no. 11; pp. 3376 - 3379
• Main Authors: Urbahns, Klaus, Woltering, Michael, Nikolic, Susanne, Pernerstorfer, Josef, Bischoff, Hilmar, Dittrich-Wengenroth, Elke, Lustig, Klemens
• Format: Journal Article
• Language: English
• Published: Elsevier Ltd 01.06.2010
• Subjects: Coronary heart disease; Human APO-A1 mice; In vivo activity; PPAR; Structure–activity relationship; Synthesis; Synthesis; PPAR; Coronary heart disease; Human APO-A1 mice; Structure–activity relationship; In vivo activity
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2010.04.019

The design, synthesis and pharmacological properties of a novel class of PPARα agonists is described. Compound 2 is a novel, potent and specific glycine amide with oral bioavailability in rodents. The compound is active in vivo and alters plasma lipids in hAPO-A1 transgenic mice after oral administration. The design, synthesis and pharmacological properties of a novel class of PPARα agonists is described. Compound 2 is a novel, potent and specific glycine amide with oral bioavailability in rodents. The compound is active in vivo and alters plasma lipids in hAPO-A1 transgenic mice after oral administration.