Design, synthesis, biological evaluation and docking studies of pterostilbene analogs inside PPARalpha.

Abstract:

:Pterostilbene, a naturally occurring analog of resveratrol, has previously shown PPARalpha activation in H4IIEC3 cells and was found to decrease cholesterol levels in animals. In this study, analogs of pterostilbene were synthesized and their ability to activate PPARalpha was investigated. Among analogs that was synthesized (E)-4-(3,5-dimethoxystyryl)phenyl dihydrogen phosphate showed activity higher than pterostilbene and control drug ciprofibrate. Docking of the stilbenes inside PPARalpha showed the presence of important hydrogen bond interactions for PPARalpha activation.

journal_name

Bioorg Med Chem

authors

Mizuno CS,Ma G,Khan S,Patny A,Avery MA,Rimando AM

doi

10.1016/j.bmc.2008.01.051

subject

Has Abstract

pub_date

2008-04-01 00:00:00

pages

3800-8

issue

7

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(08)00071-0

journal_volume

16

pub_type

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