| Autor: |
Xu, Yanping, J. Etgen, Garret, L. Broderick, Carol, Canada, Emily, Gonzalez, Isabel, Lamar, Jason, Montrose-Rafizadeh, Chahrzad, A. Oldham, Brian, J. Osborne, John, Xie, Chaoyu, Shi, Qing, L. Winneroski, Leonard, York, Jeremy, Yumibe, Nathan, Zink, Richard, Mantlo, Nathan |
| Zdroj: |
Journal of Medicinal Chemistry; September 2006, Vol. 49 Issue: 19 p5649-5652, 4p |
| Abstrakt: |
The design and synthesis of the dual peroxisome proliferator-activated receptor (PPAR) / agonist (R)-3-4-3-(4-chloro-2-phenoxy-phenoxy)-butoxy-2-ethyl-phenyl-propionic acid (20) for the treatment of type 2 diabetes and associated dyslipidemia is described. The compound possesses a potent dual hPPAR / agonist profile (IC50 19 nM/4 nM; EC50 102 nM/6 nM for hPPAR and hPPAR, respectively). In preclinical models, the compound improves insulin sensitivity and reverses diabetic hyperglycemia with less weight gain at a given level of glucose control relative to rosiglitazone. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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