title: Synthesis of new carbo- and heterocyclic analogues of 8-HETE and evaluation of their activity towards the PPARs.
abstract: A new class of dual PPARs alpha and gamma agonists was developed. These compounds are structural analogues of the arachidonic acid metabolite, the 8-(S)-HETE. A versatile strategy has been introduced to prepare the target molecules having different carbo- and heterocyclic cores and to modulate the unsaturations on the side chains. Their affinity towards the PPARs alpha and gamma receptors is reported, together with their transactivation percentage. Most of these derivatives have a good activity as dual agonists but the quinoline-derived products appear as the most promising compounds.
authors.affiliation: ENSCR, Laboratoire de Synthèse et Activation de Biomolécules, CNRS UMR 6052, Avenue du Général Leclerc, 35700 Rennes-Beaulieu, France.
authors.forename: Frédéric
authors.initials: F
authors.lastname: Caijo
authors.forename: Paul
authors.initials: P
authors.lastname: Mosset
authors.forename: René
authors.initials: R
authors.lastname: Grée
authors.forename: Valérie
authors.initials: V
authors.lastname: Audinot-Bouchez
authors.forename: Jean
authors.initials: J
authors.lastname: Boutin
authors.forename: Pierre
authors.initials: P
authors.lastname: Renard
authors.forename: Daniel-Henri
authors.initials: DH
authors.lastname: Caignard
authors.forename: Catherine
authors.initials: C
authors.lastname: Dacquet
mesh_terms: D000818:Animals; D019556:COS Cells; D004353:Drug Evaluation, Preclinical; D006893:Hydroxyeicosatetraenoic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D047493:PPAR alpha / Q000819:agonists*; D047495:PPAR gamma / Q000819:agonists*
chemical_list: D006893:Hydroxyeicosatetraenoic Acids; D047493:PPAR alpha; D047495:PPAR gamma; C047628:8-hydroxyeicosatetraenoic acid