title: 4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.
abstract: Type-2 diabetes (T2D) is a complex metabolic disease characterized by insulin resistance in the liver and peripheral tissues accompanied by a defect in pancreatic beta-cell. Since their discovery three subtypes of Peroxisomes Proliferators Activated Receptors were identified namely PPARalpha, PPARgamma and PPARbeta/(delta). We were interested in designing novel PPARgamma selective agonists and/or dual PPARalpha/gamma agonists. Based on the typical topology of synthetic PPAR agonists, we focused our design approach on 4,4-dimethyl-1,2,3,4-tetrahydroquinoline as novel cyclic tail.
authors.affiliation: SPOT-EA3857, UFR des Sciences Pharmaceutiques, 31 Avenue Monge, 37200 Tours, France.
authors.forename: Cécile
authors.initials: C
authors.lastname: Parmenon
authors.forename: Jérôme
authors.initials: J
authors.lastname: Guillard
authors.forename: Daniel-Henri
authors.initials: DH
authors.lastname: Caignard
authors.forename: Nathalie
authors.initials: N
authors.lastname: Hennuyer
authors.forename: Bart
authors.initials: B
authors.lastname: Staels
authors.forename: Valérie
authors.initials: V
authors.lastname: Audinot-Bouchez
authors.forename: Jean-Albert
authors.initials: JA
authors.lastname: Boutin
authors.forename: Catherine
authors.initials: C
authors.lastname: Dacquet
authors.forename: Alain
authors.initials: A
authors.lastname: Ktorza
authors.forename: Marie-Claude
authors.initials: MC
authors.lastname: Viaud-Massuard
mesh_terms: D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D047493:PPAR alpha / Q000819:agonists*; D047495:PPAR gamma / Q000819:agonists*; D011804:Quinolines / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: C528892:4,4-dimethyl-1,2,3,4-tetrahydroquinoline; D007004:Hypoglycemic Agents; D047493:PPAR alpha; D047495:PPAR gamma; D011804:Quinolines