Jump to main content
Jump to site search
PLANNED MAINTENANCE Close the message box

Scheduled maintenance work on Wednesday 27th March 2019 from 11:00 AM to 1:00 PM (GMT).

During this time our website performance may be temporarily affected. We apologise for any inconvenience this might cause and thank you for your patience.


Issue 8, 2015
Previous Article Next Article

PPARα agonists based on stilbene and its bioisosteres: biological evaluation and docking studies

Author affiliations

Abstract

A new series of gemfibrozil analogues conjugated with trans-stilbene were synthesized and evaluated with the aim of developing new PPARα agonists. The phenyls of stilbene were modified by introducing substituents in the ortho or para position and only the distal ring was substituted with naphthyl or heteroaromatic moieties, keeping the dimethylpentanoic skeleton of gemfibrozil unaltered. Two compounds, 5a and 5d, exhibited good activation of PPARα and were also screened for their activity on PPARα-regulated gene CPT1A. Structure-based studies carried out on the active ligands highlighted the dominant role of ligand solvation energy and hydrophobic effect in determining the PPARα activation.

Graphical abstract: PPARα agonists based on stilbene and its bioisosteres: biological evaluation and docking studies

Back to tab navigation

Supplementary files

Publication details

The article was received on 12 Apr 2015, accepted on 16 Jun 2015 and first published on 18 Jun 2015


Article type: Concise Article
DOI: 10.1039/C5MD00151J
Citation: Med. Chem. Commun., 2015,6, 1513-1517
  • Open access: Creative Commons BY-NC license
  •   Request permissions

    PPARα agonists based on stilbene and its bioisosteres: biological evaluation and docking studies

    B. De Filippis, M. Agamennone, A. Ammazzalorso, I. Bruno, A. D'Angelo, M. Di Matteo, M. Fantacuzzi, L. Giampietro, A. Giancristofaro, C. Maccallini and R. Amoroso, Med. Chem. Commun., 2015, 6, 1513
    DOI: 10.1039/C5MD00151J

    This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. Material from this article can be used in other publications provided that the correct acknowledgement is given with the reproduced material and it is not used for commercial purposes.

    Reproduced material should be attributed as follows:

    • For reproduction of material from NJC:
      [Original citation] - Published by The Royal Society of Chemistry (RSC) on behalf of the Centre National de la Recherche Scientifique (CNRS) and the RSC.
    • For reproduction of material from PCCP:
      [Original citation] - Published by the PCCP Owner Societies.
    • For reproduction of material from PPS:
      [Original citation] - Published by The Royal Society of Chemistry (RSC) on behalf of the European Society for Photobiology, the European Photochemistry Association, and RSC.
    • For reproduction of material from all other RSC journals:
      [Original citation] - Published by The Royal Society of Chemistry.

    Information about reproducing material from RSC articles with different licences is available on our Permission Requests page.

Search articles by author

Spotlight

Advertisements