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. 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

Colin M Tice  1 , Paul B Noto  1 , Kristi Yi Fan  1 , Wei Zhao  1 , Stephen D Lotesta  1 , Chengguo Dong  1 , Andrew P Marcus  1 , Ya-Jun Zheng  1 , Guozhou Chen  1 , Zhongren Wu  1 , Rebecca Van Orden  1 , Jing Zhou  1 , Yuri Bukhtiyarov  1 , Yi Zhao  1 , Kerri Lipinski  1 , Lamont Howard  1 , Joan Guo  1 , Geeta Kandpal  1 , Shi Meng  1 , Andrew Hardy  1 , Paula Krosky  1 , Richard E Gregg  1 , Katerina Leftheris  1 , Brian M McKeever  1 , Suresh B Singh  1 , Deepak Lala  1 , Gerard M McGeehan  1 , Linghang Zhuang  1 , David A Claremon  1
Affiliations

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

Colin M Tice et al. Bioorg Med Chem Lett. .

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.

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