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) a, g, and d. Three compds. displayed 56 to 96% of maximal activity of the ref. drug Wy-14643 on PPARa, and two of these, i.e., 1 and 5, exhibited also moderate activity on either PPARg or d with efficacy equal to 50% and 46% of that of rosiglitazone and GW 501516, resp. Thus, compds. 1 and 5 represent interesting starting point for prepg. novel agents for the treatment of dyslipidemia or of dyslipidemic type-2 diabetes.
[4-(2H-1,2,3-benzotriazol-2-yl)phenoxy]alkanoic acids as agonists of peroxisome proliferator-activated receptors (PPARs) / A. Sparatore, C. Godio, E. Perrino, S. Romeo, B. Staels, J.C. Fruchart, M. Crestani. - In: CHEMISTRY & BIODIVERSITY. - ISSN 1612-1872. - 3:4(2006 Apr), pp. 385-395.
Titolo: | [4-(2H-1,2,3-benzotriazol-2-yl)phenoxy]alkanoic acids as agonists of peroxisome proliferator-activated receptors (PPARs) |
Autori: | SPARATORE, ANNA CONCETTINA (Primo) GODIO, CRISTINA (Secondo) CRESTANI, MAURIZIO (Ultimo) |
Parole Chiave: | peroxisome proliferator-activated receptors (PPARs) ; 2H-1,2,3-benzotriazole derivatives ; fibrate analogues |
Settore Scientifico Disciplinare: | Settore BIO/10 - Biochimica Settore CHIM/08 - Chimica Farmaceutica |
Data di pubblicazione: | apr-2006 |
Rivista: | |
Tipologia: | Article (author) |
Digital Object Identifier (DOI): | http://dx.doi.org/10.1002/cbdv.200690042 |
Appare nelle tipologie: | 01 - Articolo su periodico |