Minor structural modifications convert a selective PPARalpha agonist into a potent, highly selective PPARdelta agonist.
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.
Weigand
Stefan
S
BAYER Health Care AG, Pharma Research, D-42096 Wuppertal, Germany. stefan.weigand@roche.com
Bischoff
Hilmar
H
Dittrich-Wengenroth
Elke
E
Heckroth
Heike
H
Lang
Dieter
D
Vaupel
Andrea
A
Woltering
Michael
M
D047493:PPAR alpha / Q000819:agonists*; D047494:PPAR delta / Q000819:agonists*; D013329:Structure-Activity Relationship
D047493:PPAR alpha; D047494:PPAR delta