Druggability profile of stilbene-derived PPAR agonists: determination of physicochemical properties and PAMPA study. Issue 11 (2nd September 2019)

• Record Type: Journal Article
• Authors: Linciano, Pasquale; De Filippis, Barbara; Ammazzalorso, Alessandra; Amoia, Pasquale; Cilurzo, Felisa; Fantacuzzi, Marialuigia; Giampietro, Letizia; Maccallini, Cristina; Petit, Charlotte; Amoroso, Rosa
• Is Part Of: MedChemComm. Volume 10:Issue 11(2019)
• Page Start: 1892
• Page End: 1899
• Publication Date: 2019-09-02
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19
• DOI: 10.1039/c9md00286c
• Languages: English
• ISSNs: 2040-2503

Abstract

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. 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.