Minor structural modifications convert a selective PPARalpha agonist into a potent, highly selective PPARdelta agonist

Stefan Weigand; Hilmar Bischoff; Elke Dittrich-Wengenroth; Heike Heckroth; Dieter Lang; Andrea Vaupel; Michael Woltering

doi:10.1016/j.bmcl.2005.06.023

Minor structural modifications convert a selective PPARalpha agonist into a potent, highly selective PPARdelta agonist

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4619-23. doi: 10.1016/j.bmcl.2005.06.023.

Authors

Stefan Weigand¹, Hilmar Bischoff, Elke Dittrich-Wengenroth, Heike Heckroth, Dieter Lang, Andrea Vaupel, Michael Woltering

Affiliation

¹ BAYER Health Care AG, Pharma Research, D-42096 Wuppertal, Germany. stefan.weigand@roche.com

PMID: 16115765
DOI: 10.1016/j.bmcl.2005.06.023

Abstract

We report the solid-phase synthesis and pharmacological evaluation of a new series of small-molecule agonists of the human peroxisome proliferator-activated receptor delta (PPARdelta) based on a lead structure from our PPARalpha program. Compound 33 showed good pharmacokinetics.

MeSH terms

PPAR alpha / agonists*
PPAR delta / agonists*
Structure-Activity Relationship

Substances

PPAR alpha
PPAR delta