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.
Original language | English |
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Pages (from-to) | 3156-3172 |
Number of pages | 17 |
Journal | Bioorganic and Medicinal Chemistry |
Volume | 19 |
Issue number | 10 |
DOIs | |
Publication status | Published - 2011 May 15 |
Externally published | Yes |
Keywords
- Molecular design
- Nuclear receptor
- PPAR agonist
- Subtype selectivity
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry