Discovery of new PPARγ agonists based on arylopeptoids

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 potentiall...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2013-07, Vol.23 (14), p.4162-4165
Main Authors: Worm-Leonhard, Kasper, Hjelmgaard, Thomas, Petersen, Rasmus K., Kristiansen, Karsten, Nielsen, John
Format: Article
Language:English
Subjects:
agonists
amides
Amides - chemical synthesis
Amides - chemistry
Amides - metabolism
Aromatic amide
bioactive properties
chemistry
Drug Evaluation, Preclinical
Humans
Library synthesis
Lifestyle diseases
Peptoids - chemistry
Peroxisome proliferator-activated receptors
PPAR gamma - agonists
PPAR gamma - metabolism
Protein Binding
receptors
Solid-phase synthesis
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Description
Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2013.05.034