Peroxisome proliferator-activated receptor agonists with phenethylphenylphthalimide skeleton derived from thalidomide-related liver X receptor antagonists: relationship between absolute configuration and subtype selectivity.

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.

journal_name

Bioorg Med Chem

authors

Motoshima K,Ishikawa M,Hashimoto Y,Sugita K

doi

10.1016/j.bmc.2011.03.065

subject

Has Abstract

pub_date

2011-05-15 00:00:00

pages

3156-72

issue

10

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(11)00254-9

journal_volume

19

pub_type

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