Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides.
Article Details
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Swahn BM, Macsari I, Viklund J, Ohberg L, Sjodin J, Neelissen J, Lindquist J
Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides.
Bioorg Med Chem Lett. 2009 Apr 1;19(7):2009-12. doi: 10.1016/j.bmcl.2009.02.039. Epub 2009 Feb 13.
- PubMed ID
- 19264481 [ View in PubMed]
- 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 LXRbeta 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) TO-901317 Oxysterols receptor LXR-alpha EC 50 (nM) 10 N/A N/A Details TO-901317 Oxysterols receptor LXR-alpha EC 50 (nM) 85 N/A N/A Details