Discovery of new PPARγ agonists based on arylopeptoids

Kasper Worm-Leonhard; Thomas Hjelmgaard; Rasmus Koefoed Petersen; Karsten Kristiansen; John Nielsen

doi:10.1016/j.bmcl.2013.05.034

Discovery of new PPARγ agonists based on arylopeptoids

Kasper Worm-Leonhard, Thomas Hjelmgaard, Rasmus Koefoed Petersen, Karsten Kristiansen, John Nielsen

8 Citations (Scopus)

Abstract

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.

Original language	English
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	23
Pages (from-to)	4162-4165
Number of pages	4
ISSN	0960-894X
DOIs	https://doi.org/10.1016/j.bmcl.2013.05.034
Publication status	Published - 15 Jul 2013

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abstract = "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.",

author = "Kasper Worm-Leonhard and Thomas Hjelmgaard and Petersen, {Rasmus Koefoed} and Karsten Kristiansen and John Nielsen",

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T1 - Discovery of new PPARγ agonists based on arylopeptoids

AU - Worm-Leonhard, Kasper

AU - Hjelmgaard, Thomas

AU - Petersen, Rasmus Koefoed

AU - Kristiansen, Karsten

AU - Nielsen, John

PY - 2013/7/15

Y1 - 2013/7/15

N2 - 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.

AB - 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.

U2 - 10.1016/j.bmcl.2013.05.034

DO - 10.1016/j.bmcl.2013.05.034

M3 - Journal article

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VL - 23

SP - 4162

EP - 4165

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

ER -

Discovery of new PPARγ agonists based on arylopeptoids

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