Synthesis and evaluation of azaindole-alpha-alkyloxyphenylpropionic acid analogues as PPARalpha/gamma agonists.
A series of azaindole-alpha-alkyloxyphenylpropionic acid analogues was synthesized and evaluated for PPAR agonist activities. Structure-activity relationship was developed for PPARalpha/gamma dual agonism. One of the synthesized compound 7a was identified as a potent, selective PPARalpha/gamma dual agonist.
Cai
Zhefeng
Z
Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.
Feng
Jun
J
Guo
Yanshen
Y
Li
Pingping
P
Shen
Zhufang
Z
Chu
Fengming
F
Guo
Zongru
Z
D000818:Animals; D002460:Cell Line; D015195:Drug Design; D006801:Humans; D066298:In Vitro Techniques; D051379:Mice; D047493:PPAR alpha / Q000819:agonists*; D047495:PPAR gamma / Q000819:agonists*; D010666:Phenylpropionates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011993:Recombinant Fusion Proteins / Q000819:agonists; D013329:Structure-Activity Relationship
D047493:PPAR alpha; D047495:PPAR gamma; D010666:Phenylpropionates; D011993:Recombinant Fusion Proteins