Issue 11, 2019

Druggability profile of stilbene-derived PPAR agonists: determination of physicochemical properties and PAMPA study

Abstract

PPAR agonists represent a new therapeutic opportunity for the prevention and treatment of neurodegenerative disorders, but their pharmacological success depends on favourable pharmacokinetic properties and capability to cross the BBB. In this study, we assayed some PPAR agonists previously synthesized by us for their physicochemical properties, with particular references to lipophilicity, solubility and permeability profiles, using the PAMPA. Although tested compounds showed high lipophilicity and low aqueous solubility, the results revealed a good overall druggability profile, encouraging further studies in the field of neurodegenerative diseases.

Graphical abstract: Druggability profile of stilbene-derived PPAR agonists: determination of physicochemical properties and PAMPA study

Supplementary files

Article information

Article type
Research Article
Submitted
20 May 2019
Accepted
12 Aug 2019
First published
15 Aug 2019

Med. Chem. Commun., 2019,10, 1892-1899

Druggability profile of stilbene-derived PPAR agonists: determination of physicochemical properties and PAMPA study

P. Linciano, B. De Filippis, A. Ammazzalorso, P. Amoia, F. Cilurzo, M. Fantacuzzi, L. Giampietro, C. Maccallini, C. Petit and R. Amoroso, Med. Chem. Commun., 2019, 10, 1892 DOI: 10.1039/C9MD00286C

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