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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 |
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cites | cdi_FETCH-LOGICAL-c380t-8efd3b074f099c885f82e49bc2d4a6afd5bf3c0f9fc1ba1c6e8b1cdbc337887f3 |
container_end_page | 4165 |
container_issue | 14 |
container_start_page | 4162 |
container_title | Bioorganic & medicinal chemistry letters |
container_volume | 23 |
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 |
format | article |
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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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