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

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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

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Publication details

The article was received on 20 May 2019, accepted on 12 Aug 2019 and first published on 15 Aug 2019


Article type: Research Article
DOI: 10.1039/C9MD00286C
Med. Chem. Commun., 2019, Advance Article

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    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, Advance Article , DOI: 10.1039/C9MD00286C

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