Premium
[4‐(2 H ‐1,2,3‐Benzotriazol‐2‐yl)phenoxy]alkanoic Acids as Agonists of Peroxisome Proliferator‐Activated Receptors (PPARs)
Author(s) -
Sparatore Anna,
Godio Cristina,
Perrino Elena,
Romeo Sergio,
Staels Bart,
Fruchart JeanCharles,
Crestani Maurizio
Publication year - 2006
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.200690042
Subject(s) - peroxisome proliferator activated receptor , chemistry , rosiglitazone , peroxisome , peroxisome proliferator , receptor , dyslipidemia , ppar agonist , pharmacology , endocrinology , medicine , stereochemistry , biochemistry , diabetes mellitus , biology
A series of [4‐(2 H ‐1,2,3‐benzotriazol‐2‐yl)phenoxy]alkanoic acids has been synthesized and tested as agonists of Peroxisome Proliferator‐Activated Receptor (PPAR) α , γ , and δ . Three compounds displayed 56 to 96% of maximal activity of the reference drug Wy‐14643 on PPAR α , and two of these, i.e. , 1 and 5 , exhibited also moderate activity on either PPAR γ or δ 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.