Abstract
Introduction of an alkylcarboxylic acid unit, which is a partial structure of endogenous peroxisome proliferator-activated receptor (PPAR) ligands, into a phenethylphenylphthalimide skeleton, which possesses liver X receptor (LXR) antagonistic activity, afforded novel PPAR ligands. The results of structure-activity relationship analysis and docking studies led us to the potent PPAR agonists 13c-e. The absolute configuration of 13c-e affects the PPAR subtype selectivity.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Cell Line
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Drug Design
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Humans
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Ligands
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Liver X Receptors
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Models, Molecular
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Orphan Nuclear Receptors / antagonists & inhibitors*
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Peroxisome Proliferator-Activated Receptors / agonists*
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Peroxisome Proliferator-Activated Receptors / chemistry
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Peroxisome Proliferator-Activated Receptors / metabolism*
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Phthalimides / chemistry*
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Phthalimides / pharmacology*
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Receptors, Cytoplasmic and Nuclear / metabolism
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Structure-Activity Relationship
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Thalidomide / chemistry*
Substances
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Ligands
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Liver X Receptors
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Orphan Nuclear Receptors
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Peroxisome Proliferator-Activated Receptors
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Phthalimides
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Receptors, Cytoplasmic and Nuclear
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farnesoid X-activated receptor
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Thalidomide