Synthesis of Aromatic Analogs of 8(S)-HETE and Their Biological Evaluation as Activators of the PPAR Nuclear Receptors

Synthesis of Aromatic Analogs of 8(S)-HETE and Their Biological Evaluation as Activators of the PPAR Nuclear Receptors

A new family of 8‐HETE analogs has been synthesized as dual PPAR α and γ agonists. A versatile strategy has been developed to allow modulations not only around the aromatic core but also on the side chains of these analogs. The affinity of these compounds towards the PPARα and PPARγ receptors is rep...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:European Journal of Organic Chemistry 2006-05, Vol.2006 (9), p.2181-2196
Hauptverfasser: Caijo, Frédéric, Mosset, Paul, Grée, René, Audinot-Bouchez, Valérie, Boutin, Jean, Renard, Pierre, Caignard, Daniel-Henri, Dacquet, Catherine
Format: Artikel
Sprache:eng
Schlagworte:
8-HETE
Diabetes
Eicosanoids
PPARs
Stereoselective synthesis
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:A new family of 8‐HETE analogs has been synthesized as dual PPAR α and γ agonists. A versatile strategy has been developed to allow modulations not only around the aromatic core but also on the side chains of these analogs. The affinity of these compounds towards the PPARα and PPARγ receptors is reported, together with their transactivation percentage. The derivatives having a propargylic type side chain gave the most promising results as dual agonists. (© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2006)
ISSN:1434-193X
1099-0690
DOI:10.1002/ejoc.200500918