Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1366576 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
Computational analysis of the ligand binding pocket of the three PPAR receptor subtypes was utilized in the design of potent PPARα agonists. Optimum PPARα potency and selectivity were obtained with substituents having van der Waals volume around 260. Compound 6 had a PPARα potency of 0.002 μM and a selectivity ratio to PPARγ and PPARδ of 410 and 2000, respectively.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Per Sauerberg, John P. Mogensen, Lone Jeppesen, Paul S. Bury, Jan Fleckner, Grith S. Olsen, Claus B. Jeppesen, Erik M. Wulff, Pavel Pihera, Miroslav Havranek, Zdenek Polivka, Ingrid Pettersson,