Synthesis and evaluation of new polyenic compounds as potential PPARs modulators.
In order to identify new leads for the treatment of type 2 diabetes, polyenic molecules A and B derived from nipecotic acid and dienol derivatives C have been prepared and their effect on PPARs transcriptional activity evaluated and compared to that of rosiglitazone, WY14,643 and GW501516. Among the synthesized compounds, dienol 39 is the most active, increasing WY14,643 PPARα response and demonstrating partial agonist properties on rosiglitazone PPARγ.
Laboratoire de Chimie Organique, ESPCI Paris Tech, CNRS, 10 rue Vauquelin, 75231-PARIS Cedex 05, France.
Dominique
D
Amans
Véronique
V
Bellosta
Catherine
C
Dacquet
Alain
A
Ktorza
Nathalie
N
Hennuyer
Bart
B
Staels
Daniel-Henri
DH
Caignard
Janine
J
Cossy
D000475:Alkenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D060326:Chemistry Techniques, Synthetic; D006801:Humans; D047492:Peroxisome Proliferator-Activated Receptors / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000235:genetics; D015533:Transcriptional Activation / Q000187:drug effects
D000475:Alkenes; D047492:Peroxisome Proliferator-Activated Receptors