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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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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
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Language:English
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cited_by cdi_FETCH-LOGICAL-c380t-8efd3b074f099c885f82e49bc2d4a6afd5bf3c0f9fc1ba1c6e8b1cdbc337887f3
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container_end_page 4165
container_issue 14
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container_title Bioorganic & medicinal chemistry letters
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creator Worm-Leonhard, Kasper
Hjelmgaard, Thomas
Petersen, Rasmus K.
Kristiansen, Karsten
Nielsen, John
description 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.
doi_str_mv 10.1016/j.bmcl.2013.05.034
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ispartof Bioorganic & medicinal chemistry letters, 2013-07, Vol.23 (14), p.4162-4165
issn 0960-894X
1464-3405
language eng
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source Elsevier
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
title Discovery of new PPARγ agonists based on arylopeptoids
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