| Autor: |
Xu Y; Lilly Research Laboratories, A Division of Eli Lilly & Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA. xu_yanping@lilly.com, Rito CJ, Etgen GJ, Ardecky RJ, Bean JS, Bensch WR, Bosley JR, Broderick CL, Brooks DA, Dominianni SJ, Hahn PJ, Liu S, Mais DE, Montrose-Rafizadeh C, Ogilvie KM, Oldham BA, Peters M, Rungta DK, Shuker AJ, Stephenson GA, Tripp AE, Wilson SB, Winneroski LL, Zink R, Kauffman RF, McCarthy JR |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2004 May 06; Vol. 47 (10), pp. 2422-5. |
| DOI: |
10.1021/jm0342616 |
| Abstrakt: |
The design and synthesis of the dual peroxisome proliferator activated receptor (PPAR) alpha/gamma agonist (S)-2-methyl-3-[4-[2-(5-methyl-2-thiophen-2-yl-oxazol-4-yl)ethoxy]phenyl]-2-phenoxypropionic acid (2) for the treatment of type 2 diabetes and associated dyslipidemia are described. 2 possesses a potent dual hPPAR alpha/gamma agonist profile (IC(50) = 28 and 10 nM; EC(50) = 9 and 4 nM, respectively, for hPPARalpha and hPPARgamma). In preclinical models, 2 substantially improves insulin sensitivity and potently reverses diabetic hyperglycemia while significantly improving overall lipid homeostasis. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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