title: Discovery of new PPARγ agonists based on arylopeptoids.
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.
authors.affiliation: Department of Chemistry, Section for Chemical Biology and Nanobioscience, Faculty of Science, University of Copenhagen, Thorvaldsensvej 40, 1871 Frederiksberg C, Denmark.
authors.forename: Kasper
authors.initials: K
authors.lastname: Worm-Leonhard
authors.forename: Thomas
authors.initials: T
authors.lastname: Hjelmgaard
authors.forename: Rasmus K
authors.initials: RK
authors.lastname: Petersen
authors.forename: Karsten
authors.initials: K
authors.lastname: Kristiansen
authors.forename: John
authors.initials: J
authors.lastname: Nielsen
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism; D004353:Drug Evaluation, Preclinical; D006801:Humans; D047495:PPAR gamma / Q000819:agonists* / Q000378:metabolism; D034444:Peptoids / Q000737:chemistry*; D011485:Protein Binding
chemical_list: D000577:Amides; D047495:PPAR gamma; D034444:Peptoids