| Autor: |
Shi Q; Eli Lilly and Company, Lilly Research Labs, Lilly Corporate Center, Indianapolis, IN 46285, USA. shi_qing@lilly.com, Canada EJ, Xu Y, Warshawsky AM, Etgen GJ, Broderick CL, Clutinger CK, Irwin LA, Laurila ME, Montrose-Rafizadeh C, Oldham BA, Wang M, Winneroski LL, Xie C, York JS, Yumibe NP, Zink RW, Mantlo N |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Dec 15; Vol. 17 (24), pp. 6744-9. Date of Electronic Publication: 2007 Oct 18. |
| DOI: |
10.1016/j.bmcl.2007.10.047 |
| Abstrakt: |
A series of potent amide linked PPARgamma/delta dual agonists (1a) has been discovered through rational design. In the ZDF rat model of type 2 diabetes, compound (R)-3-[4-(3-{1-[(5-chloro-1,3-dimethyl-1H-indole-2-carbonyl)-amino]-ethyl}-5-fluoro-phenoxy)-2-ethyl-phenyl]-propionic acid (42) from this series has demonstrated glucose lowering efficacy comparable to the marketed PPARgamma agonist rosiglitazone with less weight gain. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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