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Bioorg Med Chem Lett. 2016 Oct 15;26(20):5044-5050. doi: 10.1016/j.bmcl.2016.08.089. Epub 2016 Aug 29.

Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.

Author information

1
Vitae Pharmaceuticals, 502 West Office Center Drive, Fort Washington, PA 19034, USA.

Abstract

Liver X receptor (LXR) agonists have been reported to lower brain amyloid beta (Aβ) and thus to have potential for the treatment of Alzheimer's disease. Structure and property based design led to the discovery of a series of orally bioavailable, brain penetrant LXR agonists. Oral administration of compound 18 to rats resulted in significant upregulation of the expression of the LXR target gene ABCA1 in brain tissue, but no significant effect on Aβ levels was detected.

KEYWORDS:

Alzheimer’s disease; Brain; LXR; Structure-based drug design

PMID:
27599745
DOI:
10.1016/j.bmcl.2016.08.089
[Indexed for MEDLINE]

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