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Open AccessCommunication
Mar. Drugs 2016, 14(6), 112; doi:10.3390/md14060112

Synthesis of Phthalimide Derivatives as Potential PPAR-γ Ligands

1
College of Pharmacy, Pusan National University, Busan 46241, Korea
2
College of Pharmacy, Kyung Hee University, Seoul 02447, Korea
These authors equally contributed to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Orazio Taglialatela-Scafati
Received: 1 April 2016 / Revised: 27 May 2016 / Accepted: 30 May 2016 / Published: 8 June 2016
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Abstract

Paecilocin A, a phthalide derivative isolated from the jellyfish-derived fungus Paecilomyces variotii, activates PPAR-γ (Peroxisome proliferator-activated receptor gamma) in rat liver Ac2F cells. Based on a SAR (Structure-activity relationships) study and in silico analysis of paecilocin A-mimetic derivatives, additional N-substituted phthalimide derivatives were synthesized and evaluated for PPAR-γ agonistic activity in both murine liver Ac2F cells and in human liver HepG2 cells by luciferase assay, and for adipogenic activity in 3T3-L1 cells. Docking simulation indicated PD6 was likely to bind most strongly to the ligand binding domain of PPAR-γ by establishing crucial H-bonds with key amino acid residues. However, in in vitro assays, PD1 and PD2 consistently displayed significant PPAR-γ activation in Ac2F and HepG2 cells, and adipogenic activity in 3T3-L1 preadipocytes. View Full-Text
Keywords: PPAR-γ agonist; paecilocin A; type 2 diabetes; phthalimide; adipogenesis; 3T3-L1 PPAR-γ agonist; paecilocin A; type 2 diabetes; phthalimide; adipogenesis; 3T3-L1
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Eom, S.H.; Liu, S.; Su, M.; Noh, T.H.; Hong, J.; Kim, N.D.; Chung, H.Y.; Yang, M.H.; Jung, J.H. Synthesis of Phthalimide Derivatives as Potential PPAR-γ Ligands. Mar. Drugs 2016, 14, 112.

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