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.

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 15; no. 20; pp. 4619 - 4623
Main Authors Weigand, Stefan, Bischoff, Hilmar, Dittrich-Wengenroth, Elke, Heckroth, Heike, Lang, Dieter, Vaupel, Andrea, Woltering, Michael
Format Journal Article
LanguageEnglish
Published England 15.10.2005
Subjects
PPAR alpha - agonists
PPAR delta - agonists
Structure-Activity Relationship
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Summary: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.
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ISSN:0960-894X