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

Journal Article · · Bioorganic and Medicinal Chemistry Letters
Not Available
Sponsoring Organization:
USDOE Office of Science (SC), Basic Energy Sciences (BES)
Grant/Contract Number:
AC02-98CH10886
OSTI ID:
1396353
Journal Information:
Bioorganic and Medicinal Chemistry Letters, Journal Name: Bioorganic and Medicinal Chemistry Letters Journal Issue: 20 Vol. 26; ISSN 0960-894X
Publisher:
ElsevierCopyright Statement
Country of Publication:
United Kingdom
Language:
English

References (29)

Liver X Receptor Agonist Modifies the DNA Methylation Profile of Synapse and Neurogenesis-Related Genes in the Triple Transgenic Mouse Model of Alzheimer’s Disease journal November 2015
Different roles of liver X receptor α and β in lipid metabolism: Effects of an α-selective and a dual agonist in mice deficient in each subtype journal February 2006
Broad-Spectrum Therapeutic Suppression of Metastatic Melanoma through Nuclear Hormone Receptor Activation journal February 2014
Liver X receptor and retinoid X receptor agonists inhibit inflammatory responses of microglia and astrocytes journal February 2007
The LXR agonist TO901317 selectively lowers hippocampal Aβ42 and improves memory in the Tg2576 mouse model of Alzheimer's disease journal April 2007
LXR activation protects hippocampal microvasculature in very old triple transgenic mouse model of Alzheimer’s disease journal May 2016
Liver X receptor activation restores memory in aged AD mice without reducing amyloid journal July 2011
ApoE Promotes the Proteolytic Degradation of Aβ journal June 2008
Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist journal March 2016
Identification and in Vivo Evaluation of Liver X Receptor β-Selective Agonists for the Potential Treatment of Alzheimer’s Disease journal March 2016
Moving beyond Rules: The Development of a Central Nervous System Multiparameter Optimization (CNS MPO) Approach To Enable Alignment of Druglike Properties journal March 2010
Structure-mutagenicity relationships of N-oxidized derivatives of aniline, o-toluidine, 2'-methyl-4-aminobiphenyl, and 3,2'-dimethyl-4-aminobiphenyl journal August 1979
The Medicinal Chemistry of Liver X Receptor (LXR) Modulators journal May 2014
Liver X receptors in lipid metabolism: opportunities for drug discovery journal May 2014
Dialkylbiaryl phosphines in Pd-catalyzed amination: a user's guide journal January 2011
Design of potential new HIV protease inhibitors: enantioconvergent synthesis of new pyrrolidin-3-ol, and pyrrolidin-3-one peptide conjugates
  • Courcambeck, Jérôme; Bihel, Frédéric; De Michelis, Céline
  • Journal of the Chemical Society, Perkin Transactions 1, Issue 12 https://doi.org/10.1039/b101584m
journal January 2001
Liver X Receptor Activators Display Anti-Inflammatory Activity in Irritant and Allergic Contact Dermatitis Models: Liver-X-Receptor-Specific Inhibition of Inflammation and Primary Cytokine Production journal February 2003
Attenuation of neuroinflammation and Alzheimer's disease pathology by liver x receptors journal June 2007
Structural requirements of ligands for the oxysterol liver X receptors LXR  and LXR  journal January 1999
ATP-binding Cassette Transporter A1 Mediates the Beneficial Effects of the Liver X Receptor Agonist GW3965 on Object Recognition Memory and Amyloid Burden in Amyloid Precursor Protein/Presenilin 1 Mice* journal October 2010
The Liver X Receptor Ligand T0901317 Decreases Amyloid β Production in Vitro and in a Mouse Model of Alzheimer's Disease journal February 2005
Assessment of the Medicines Lidocaine, Prilocaine, and Their Metabolites, 2,6-Dimethylaniline and 2-Methylaniline, for DNA Adduct Formation in Rat Tissues journal May 2008
Ligand activation of LXRβ reverses atherosclerosis and cellular cholesterol overload in mice lacking LXRα and apoE journal August 2007
Systemic treatment with liver X receptor agonists raises apolipoprotein E, cholesterol, and amyloid-β peptides in the cerebral spinal fluid of rats journal January 2010
Regulation of Cholesterol Homeostasis by the Liver X Receptors in the Central Nervous System journal June 2002
Effect of LXR/RXR agonism on brain and CSF Aβ40 levels in rats journal February 2016
Role of Liver X Receptor in AD Pathophysiology journal December 2015
Liver X Receptor Agonist Treatment Ameliorates Amyloid Pathology and Memory Deficits Caused by High-Fat Diet in APP23 Mice journal May 2010
Critical Role of Astroglial Apolipoprotein E and Liver X Receptor-  Expression for Microglial A  Phagocytosis journal May 2011

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