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Synthesis of Aromatic Analogs of 8( S )‐HETE and Their Biological Evaluation as Activators of the PPAR Nuclear Receptors
Author(s) -
Caijo Frédéric,
Mosset Paul,
Grée René,
AudinotBouchez Valérie,
Boutin Jean,
Renard Pierre,
Caignard DanielHenri,
Dacquet Catherine
Publication year - 2006
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.200500918
Subject(s) - chemistry , transactivation , nuclear receptor , side chain , receptor , peroxisome proliferator activated receptor , stereochemistry , combinatorial chemistry , biochemistry , organic chemistry , transcription factor , gene , polymer
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)