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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis of a Novel Series of 8-HETE Analogs and their Biological Evaluation Towards the PPAR Nuclear Receptors

Author(s): Melanie Liutkus, Catherine Dacquet, Valerie Audinot-Bouchez, Jean Boutin, Daniel-Henri Caignard, Alain Ktorza and Rene Gree

Volume 5, Issue 8, 2008

Page: [503 - 511] Pages: 9

DOI: 10.2174/157018008786898572

Price: $65


A novel series of dual PPARα/γ agonists was designed through the modification of our previously described family of 8-HETE analogs. The combination of the structural elements of this family and of the classical PPAR ligands produced compounds with a quinoxaline core and two sides chains. Structure-activity relationship studies have been carried out on the new series and compounds belonging to this new family have been tested in vitro on both subtypes of PPAR nuclear receptors. Corresponding results indicated a strong decrease in the activity towards both subtypes, especially on PPARγ. However, they have also clearly shown the central role of the bottom side chain in the activity.

Keywords: PPARs, Diabetes, 8-HETE Analogs, Quinoxaline

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