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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.

SUBMITTER: Linciano P

PROVIDER: S-EPMC7069374 | biostudies-literature | 2019 Nov

REPOSITORIES: biostudies-literature

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

Linciano Pasquale P De Filippis Barbara B Ammazzalorso Alessandra A Amoia Pasquale P Cilurzo Felisa F Fantacuzzi Marialuigia M Giampietro Letizia L Maccallini Cristina C Petit Charlotte C Amoroso Rosa R

MedChemComm 20190815 11

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 a ...[more]

PMID: 32206235

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