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.
Druggability profile of stilbene-derived PPAR agonists: Determination of physicochemical properties and PAMPA study
Linciano P.;De Filippis B.;Ammazzalorso A.;Amoia P.;Cilurzo F.;Fantacuzzi M.;Giampietro L.;Maccallini C.;Amoroso R.
2019-01-01
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
