Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRβ and low blood-brain penetration
A series of quinoline-3-carboxamide containing sulfones was prepared and found to have good binding affinity for LXRβ and moderate binding selectivity over LXRα. The 8-Cl quinoline analog 33 with a high TPSA score, displayed 34-fold binding selectivity for LXRβ over LXRα (LXRβ IC50 = 16 nM), good activity for inducing ABCA1 gene expression in a THP macrophage cell line, desired weak potency in the LXRα Gal4 functional assay, and low blood-brain barrier penetration in rat.
There is provided compounds of formula (I) wherein W is an optionally substituted aryl or heteroaryl group, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a lipoxygenase (e.g. 15- lipoxygenase) is desired and/or required, and particularly in the treatment of inflammation.
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Page/Page column 43
(2008/06/13)
Synthesis of fluoro-4-hydroxyquinoline-3-carboxylic acids by the Gould-Jacobs reaction
The synthesis of several fluoro-4-hydroxyquinoline-3-carboxylic acids by the Gould-Jacobs reaction is presented. These quinolines are important intermediates for the preparation of antibacterial fluoroquinolones.
Leyva, Elisa,Monreal, Elena,Hernandez, Alma
p. 7 - 10
(2007/10/03)
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