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Article Dans Une Revue Pharmaceutics Année : 2023

New Hybrid Compounds Incorporating Natural Products as Multifunctional Agents against Alzheimer’s Disease

Lidia Ciccone
Caterina Camodeca
Nicolò Tonali
Lucia Barlettani
Armando Rossello
  • Fonction : Auteur
Julia Kaffy
  • Fonction : Auteur
Giovanni Petrarolo
Concettina La Motta
Susanna Nencetti
Elisabetta Orlandini
  • Fonction : Auteur

Résumé

A series of new hybrid derivatives 1a–c, 2a–c, 3a–c, 4a–c, 5a–c, inspired by nature, were synthesized and studied as multifunctional agents for the treatment of Alzheimer’s disease (AD). These compounds were designed to merge together the trifluoromethyl benzyloxyaminic bioactive moiety, previously identified, with different acids available in nature. The ability of the synthesized compounds to chelate biometals, such as Cu2+, Zn2+ and Fe2+, was studied by UV–Vis spectrometer, and through a preliminary screening their antioxidant activity was evaluated by DPPH. Then, selected compounds were tested by in vitro ABTS free radical method and ex vivo rat brain TBARS assay. Compounds 2a–c, combining the strongest antioxidant and biometal chelators activities, were studied for their ability to contrast Aβ1-40 fibrillization process. Finally, starting from the promising profile obtained for compound 2a, we evaluated if it could be able to induce a positive cross-interaction between transthyretin (TTR) and Aβ in presence and in absence of Cu2+.

Dates et versions

hal-04456200 , version 1 (13-02-2024)

Identifiants

Citer

Lidia Ciccone, Caterina Camodeca, Nicolò Tonali, Lucia Barlettani, Armando Rossello, et al.. New Hybrid Compounds Incorporating Natural Products as Multifunctional Agents against Alzheimer’s Disease. Pharmaceutics, 2023, 15 (10), pp.2369. ⟨10.3390/pharmaceutics15102369⟩. ⟨hal-04456200⟩
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