TY - JOUR
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
SN - 0960-894X
VL - 23
SP - 4162
EP - 4165
JO - Bioorganic & Medicinal Chemistry Letters
JF - Bioorganic & Medicinal Chemistry Letters
ER -