Next Article in Journal
Nutraceuticals and Bioactive Components from Fish for Dyslipidemia and Cardiovascular Risk Reduction
Previous Article in Journal
Enzymatic Hydrolysis of Alginate to Produce Oligosaccharides by a New Purified Endo-Type Alginate Lyase
Article Menu

Export Article

Open AccessCommunication
Mar. Drugs 2016, 14(6), 112;

Synthesis of Phthalimide Derivatives as Potential PPAR-γ Ligands

College of Pharmacy, Pusan National University, Busan 46241, Korea
College of Pharmacy, Kyung Hee University, Seoul 02447, Korea
Authors to whom correspondence should be addressed.
These authors equally contributed to this work.
Academic Editor: Orazio Taglialatela-Scafati
Received: 1 April 2016 / Revised: 27 May 2016 / Accepted: 30 May 2016 / Published: 8 June 2016
PDF [2896 KB, uploaded 8 June 2016]


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

Figure 1

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).

Share & Cite This Article

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.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Mar. Drugs EISSN 1660-3397 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top