[4-(2H-1,2,3-benzotriazol-2-yl)phenoxy]alkanoic acids as agonists of peroxisome proliferator-activated receptors (PPARs).
A series of [4-(2H-1,2,3-benzotriazol-2-yl)phenoxy]alkanoic acids has been synthesized and tested as agonists of Peroxisome Proliferator-Activated Receptor (PPAR) alpha, gamma, and delta. Three compounds displayed 56 to 96% of maximal activity of the reference drug Wy-14643 on PPARalpha, and two of these, i.e., 1 and 5, exhibited also moderate activity on either PPARgamma or delta with efficacy equal to 50% and 46% of that of rosiglitazone and GW 501516, respectively. Thus, compounds 1 and 5 represent interesting starting point for preparing novel agents for the treatment of dyslipidemia or of dyslipidemic type-2 diabetes.
Sparatore
Anna
A
Istituto di Chimica Farmaceutica e Tossicologica, Università di Milano, Viale Abruzzi 42, I-20131 Milan. anna.sparatore@unimi.it
Godio
Cristina
C
Perrino
Elena
E
Romeo
Sergio
S
Staels
Bart
B
Fruchart
Jean-Charles
JC
Crestani
Maurizio
M
D045744:Cell Line, Tumor; D006801:Humans; D000960:Hypolipidemic Agents / Q000737:chemistry / Q000494:pharmacology; D047492:Peroxisome Proliferator-Activated Receptors / Q000819:agonists* / Q000502:physiology; D014230:Triazoles / Q000737:chemistry* / Q000494:pharmacology
D000960:Hypolipidemic Agents; D047492:Peroxisome Proliferator-Activated Receptors; D014230:Triazoles; C012771:benzotriazole