| Autor: |
Sauerberg P; Novo Nordisk A/S, Novo Nordisk Park, 2760 Måløv, Denmark., Mogensen JP, Jeppesen L, Bury PS, Fleckner J, Olsen GS, Jeppesen CB, Wulff EM, Pihera P, Havranek M, Polivka Z, Pettersson I |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Jun 01; Vol. 17 (11), pp. 3198-202. Date of Electronic Publication: 2007 Mar 12. |
| DOI: |
10.1016/j.bmcl.2007.03.015 |
| Abstrakt: |
Computational analysis of the ligand binding pocket of the three PPAR receptor subtypes was utilized in the design of potent PPARalpha agonists. Optimum PPARalpha potency and selectivity were obtained with substituents having van der Waals volume around 260. Compound 6 had a PPARalpha potency of 0.002 microM and a selectivity ratio to PPARgamma and PPARdelta of 410 and 2000, respectively. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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