Glycine amides as PPARalpha agonists

Klaus Urbahns; Michael Woltering; Susanne Nikolic; Josef Pernerstorfer; Hilmar Bischoff; Elke Dittrich-Wengenroth; Klemens Lustig

doi:10.1016/j.bmcl.2010.04.019

Glycine amides as PPARalpha agonists

Bioorg Med Chem Lett. 2010 Jun 1;20(11):3376-9. doi: 10.1016/j.bmcl.2010.04.019. Epub 2010 Apr 13.

Authors

Klaus Urbahns¹, Michael Woltering, Susanne Nikolic, Josef Pernerstorfer, Hilmar Bischoff, Elke Dittrich-Wengenroth, Klemens Lustig

Affiliation

¹ Department of Medicinal Chemistry, Bayer Healthcare, Bayer-Schering Pharma, D-42096 Wuppertal, Germany. Klaus.Urbahns@astrazeneca.com

PMID: 20452212
DOI: 10.1016/j.bmcl.2010.04.019

Abstract

The design, synthesis and pharmacological properties of a novel class of PPARalpha 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.

MeSH terms

Animals
Biological Availability
Glycine / analogs & derivatives*
Glycine / pharmacokinetics
Glycine / pharmacology
Mice
Mice, Transgenic
PPAR alpha / agonists*
Structure-Activity Relationship

Substances

PPAR alpha
glycine amide
Glycine