Marine Drugs p. 926 - 939 (2014)
Update date:2022-07-30
Topics: Retrosynthetic analysis Purification and characterization Literature Review Design of Analogs Synthesis of Key Intermediates Assembly of the Target Compounds Biological Evaluation Structure-Activity Relationship (SAR) Study Safety and Toxicity Assessment In Vivo Studies Lead Optimization Patent and Publication
Xiao, Bin
Su, Mingzhi
Kim, Eun La
Hong, Jongki
Chung, Hae Young
Kim, Hyung Sik
Yin, Jun
Jung, Jee H.
A series of N-substituted phthalimide derivatives were synthesized based on a pharmacophore study of paecilocin A (a natural PPAR-γ agonist) and synthetic leads. The introduction of hydrophilic and hydrophobic groups to the phthalimide skeleton yielded compounds 3-14. Compound 7 showed significant PPAR-γ activation in a luciferase assay using rat liver Ac2F cells. Docking simulations showed that a free hydroxyl group on the phthalimide head and a suitable hydrophilic tail, including a phenyl linker, were beneficial for PPAR-γ activation. Compound 7 and rosiglitazone concentration-dependently activated PPAR-γ with EC50 values of 0.67 μM and 0.028 μM, respectively. These phthalimide derivatives could be further investigated as a new class of PPAR-γ ligands.
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