Discovery of new PPARγ agonists based on arylopeptoids
2013
Worm-Leonhard, Kasper | Hjelmgaard, Thomas | Petersen, Rasmus K. | Kristiansen, Karsten | Nielsen, John
In this study we present the design, synthesis and biological evaluation of a small, first-generation library of small molecule aromatic amides based on the arylopeptoid skeleton. The compounds were efficiently synthesized using a highly convenient submonomer solid-phase methodology which potentially allows for access to great product diversity. The synthesized compounds were tested for their ability to activate peroxisome proliferator-activated receptors (PPARs) and they all acted as PPARγ agonists in the μM range spanning from 2.5- to 14.7-fold activation of the receptor. This is the first discovery of bioactive molecules based on the arylopeptoid architecture.
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