Design, synthesis, and evaluation of 2-alkoxydihydrocinnamates as PPAR agonists.
A series of 2-alkoxydihydrocinnamates were synthesized as PPARgamma and PPARalpha dual agonists. In vitro studies in cell model showed that these compounds were efficacious. Compound 1g was found to be a potent PPARalpha/gamma dual agonist and will be further evaluated for the treatment of type II diabetes.
Lu
Ying
Y
Department of Synthetic Medicinal Chemistry, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China.
Guo
Zongru
Z
Guo
Yanshen
Y
Feng
Jun
J
Chu
Fengming
F
D002460:Cell Line; D002934:Cinnamates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D006801:Humans; D066298:In Vitro Techniques; D008958:Models, Molecular; D015394:Molecular Structure; D047493:PPAR alpha / Q000819:agonists*; D047495:PPAR gamma / Q000819:agonists*; D011487:Protein Conformation; D017433:Protein Structure, Secondary; D021281:Quantitative Structure-Activity Relationship
D002934:Cinnamates; D047493:PPAR alpha; D047495:PPAR gamma