| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1375303 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
Abstract
The synthesis and SAR of a new series of LXR agonist is reported. The N-Aryl-3,3,3-trifluoro-2-hydroxy-2-methyl-propionamide hits were found in a limited screen of the AstraZeneca compound collection. The effort to optimize these hits into LXRβ selectivity is described. Compound 20 displayed desirable pharmacokinetic profile and up regulation of ABCA1 and ABCG1 mRNA in the brain were achieved when evaluated in vivo in mice.
Graphical abstractThe synthesis and SAR of new liver X receptor agonists is reported. The effort to optimize these hits into LXRβ selectivity is described. Compound 20 displayed desirable pharmacokinetic profile and was evaluated in vivo.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Britt-Marie Swahn, Istvan Macsari, Jenny Viklund, Liselotte Öhberg, Johanna Sjödin, Jan Neelissen, Johanna Lindquist,