Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 14, Pages 4162-4165Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.05.034
Keywords
Lifestyle diseases; Peroxisome proliferator-activated receptors; Aromatic amide; Solid-phase synthesis; Library synthesis
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Funding
- Lundbeck Foundation
- Aase and Ejnar Daninielsens Foundation
- Augustinus Foundation
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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 PPAR gamma agonists in the mu M 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. (C) 2013 Elsevier Ltd. All rights reserved.
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