Structure–activity relationships of dimeric PPAR agonists

The SAR of dimeric PPAR agonists is reported. A series of dimeric PPAR agonists were designed and tested for PPAR activity in vitro. The SAR showed that dimeric ligands with a common group or full dimeric ligands had retained or even increased PPARγ potency. The dimeric agonist concept can be used t...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2005-03, Vol.15 (5), p.1497-1500
Main Authors: Sauerberg, Per, Mogensen, John P., Jeppesen, Lone, Svensson, L. Anders, Fleckner, Jan, Nehlin, Jan, Wulff, Erik M., Pettersson, Ingrid
Format: Article
Language:English
Subjects:
Biological and medical sciences
Dimerization
Drug Design
General and cellular metabolism. Vitamins
Humans
Ligands
Medical sciences
Models, Molecular
Molecular Structure
Peroxisome Proliferator-Activated Receptors - agonists
Peroxisome Proliferator-Activated Receptors - chemistry
Pharmacology. Drug treatments
Structure-Activity Relationship
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Summary:The SAR of dimeric PPAR agonists is reported. A series of dimeric PPAR agonists were designed and tested for PPAR activity in vitro. The SAR showed that dimeric ligands with a common group or full dimeric ligands had retained or even increased PPARγ potency. The dimeric agonist concept can be used to fine tune the subtype selectivity of PPAR agonists. The PPARγ potency could, at least partly, be explained using molecular modeling.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.12.084