4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.
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.
Parmenon
Cécile
C
SPOT-EA3857, UFR des Sciences Pharmaceutiques, 31 Avenue Monge, 37200 Tours, France.
Guillard
Jérôme
J
Caignard
Daniel-Henri
DH
Hennuyer
Nathalie
N
Staels
Bart
B
Audinot-Bouchez
Valérie
V
Boutin
Jean-Albert
JA
Dacquet
Catherine
C
Ktorza
Alain
A
Viaud-Massuard
Marie-Claude
MC
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
C528892:4,4-dimethyl-1,2,3,4-tetrahydroquinoline; D007004:Hypoglycemic Agents; D047493:PPAR alpha; D047495:PPAR gamma; D011804:Quinolines