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Design and synthesis of marine fungal phthalide derivatives as PPAR-γ agonists.

Abstract：

:On the basis of a marine fungal phthalide (paecilocin A) skeleton, we synthesized 20 analogs and evaluated them for peroxisome proliferator-activated receptor gamma (PPAR-γ) binding and activation. Among these analogs, 6 and 7 had significant PPAR-γ binding activity, and 7 showed further PPAR-γ activation in rat liver Ac2F cells. In docking simulation, 7 formed H bonds with key amino acid residues of the PPAR-γ binding domain, and the overall positioning was similar to rosiglitazone. This new phthalide derivative is considered an interesting new molecular class of PPAR-γ ligands.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Xiao B,Yin J,Park M,Liu J,Li JL,Kim EL,Hong J,Chung HY,Jung JH

doi

10.1016/j.bmc.2012.06.039

subject

Has Abstract

pub_date

2012-08-15 00:00:00

pages

4954-61

issue

16

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(12)00517-2

journal_volume

20

pub_type

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