1639899-74-3Relevant academic research and scientific papers
Synthesis of PPAR-γ activators inspired by the marine natural product, paecilocin A
Xiao, Bin,Su, Mingzhi,Kim, Eun La,Hong, Jongki,Chung, Hae Young,Kim, Hyung Sik,Yin, Jun,Jung, Jee H.
, p. 926 - 939 (2014/03/21)
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.
