63010-69-5Relevant articles and documents
Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRβ and low blood-brain penetration
Hu, Baihua,Bernotas, Ron,Unwalla, Rayomand,Collini, Michael,Quinet, Elaine,Feingold, Irene,Goos-Nilsson, Annika,Wilhelmsson, Anna,Nambi, Ponnal,Evans, Mark,Wrobel, Jay
scheme or table, p. 689 - 693 (2010/06/14)
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.
Synthesis of fluoro-4-hydroxyquinoline-3-carboxylic acids by the Gould-Jacobs reaction
Leyva, Elisa,Monreal, Elena,Hernandez, Alma
, p. 7 - 10 (2007/10/03)
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.