Literature DB >> 19264481

Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides.

Britt-Marie Swahn1, Istvan Macsari, Jenny Viklund, Liselotte Ohberg, Johanna Sjödin, Jan Neelissen, Johanna Lindquist.   

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.

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Year:  2009        PMID: 19264481     DOI: 10.1016/j.bmcl.2009.02.039

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

1.  Identifying selective agonists targeting LXRβ from terpene compounds of alismatis rhizoma.

Authors:  Chuanjiong Lin; Jianzong Li; Chuanfang Wu; Jinku Bao
Journal:  J Mol Model       Date:  2021-02-22       Impact factor: 1.810

2.  Small molecule inducers of ABCA1 and apoE that act through indirect activation of the LXR pathway.

Authors:  Jianjia Fan; Rui Qi Zhao; Cameron Parro; Wenchen Zhao; Hsien-Ya Chou; Jerome Robert; Tarek Z Deeb; Carina Raynoschek; Samantha Barichievy; Ola Engkvist; Marcello Maresca; Ryan Hicks; Johan Meuller; Stephen J Moss; Nicholas J Brandon; Michael W Wood; Iva Kulic; Cheryl L Wellington
Journal:  J Lipid Res       Date:  2018-03-21       Impact factor: 5.922

3.  Synthesis and In Vitro Evaluation of Novel Liver X Receptor Agonists Based on Naphthoquinone Derivatives.

Authors:  Tatsuma Nishioka; Kaori Endo-Umeda; Yuki Ito; Akane Shimoda; Atsuko Takeuchi; Chisato Tode; Yoshihisa Hirota; Naomi Osakabe; Makoto Makishima; Yoshitomo Suhara
Journal:  Molecules       Date:  2019-11-26       Impact factor: 4.411

Review 4.  The challenges and promise of targeting the Liver X Receptors for treatment of inflammatory disease.

Authors:  Michael B Fessler
Journal:  Pharmacol Ther       Date:  2017-07-16       Impact factor: 12.310

  4 in total

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