Synthesis and evaluation of lipoic acid - donepezil hybrids for Alzheimer's disease using a straightforward strategy.

Acetylcholinesterase Alzheimer disease Antioxidant Donepezil Lipoic acid Neuroprotection

Journal

Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377

Informations de publication

Date de publication:
31 Aug 2024
Historique:
received: 13 06 2024
revised: 13 08 2024
accepted: 27 08 2024
medline: 3 9 2024
pubmed: 3 9 2024
entrez: 2 9 2024
Statut: aheadofprint

Résumé

Alzheimer's disease is associated with a progressive loss of neurons and synaptic connections in the cholinergic system. Oxidative stress contributes to neuronal damages and to the development of amyloid plaques and neurofibrillary tangles. Therefore, antioxidants have been widely studied to mitigate the progression of Alzheimer's disease, and among these, lipoic acid has demonstrated a neuroprotective effect. Here, we present the synthesis, the molecular modelling, and the evaluation of lipoic acid-donepezil hybrids based on O-desmethyldonepezil. As compounds 5 and 6 display a high inhibition of acetylcholinesterase (IC

Identifiants

pubmed: 39222891
pii: S0960-894X(24)00340-8
doi: 10.1016/j.bmcl.2024.129938
pii:
doi:

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

129938

Informations de copyright

Copyright © 2024. Published by Elsevier Ltd.

Déclaration de conflit d'intérêts

Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Auteurs

Vincent Luzet (V)

Université de Franche-Comté, FEMTO-ST, F-25000 Besançon, France. Electronic address: vincent.luzet@femto-st.fr.

Florentin Allemand (F)

Université de Franche-Comté, Chrono-environnement UMR6249, CNRS, F-25000 Besançon, France. Electronic address: florentin.allemand@edu.univ-fcomte.fr.

Chloé Richet (C)

Université de Franche-Comté, Chrono-environnement UMR6249, CNRS, F-25000 Besançon, France. Electronic address: chloe.richet@femto-st.fr.

Barbara Dehecq (B)

Université de Franche-Comté, UMR RIGHT, EFS, INSERM, F-25000 Besançon, France. Electronic address: barbara.dehecq@univ-fcomte.fr.

Alexandre Bonet (A)

Université de Franche-Comté, UMR RIGHT, EFS, INSERM, F-25000 Besançon, France. Electronic address: alexandre.bonet@univ-fcomte.fr.

Dominique Harakat (D)

URCATech, ICMR, CNRS UMR 7312, URCA Bât 18, BP 1039, 51687 Reims Cedex 2, France. Electronic address: dominique.harakat@univ-reims.fr.

Bernard Refouvelet (B)

Université de Franche-Comté, UMR INSERM 1322 LINC, F-25030 Besançon Cedex, France. Electronic address: bernard.refouvelet@univ-fcomte.fr.

Hélène Martin (H)

Université de Franche-Comté, UMR RIGHT, EFS, INSERM, F-25000 Besançon, France. Electronic address: helene.martin@univ-fcomte.fr.

Bruno Cardey (B)

Université de Franche-Comté, Chrono-environnement UMR6249, CNRS, F-25000 Besançon, France. Electronic address: bruno.cardey@univ-fcomte.fr.

Marc Pudlo (M)

Université de Franche-Comté, UMR RIGHT, EFS, INSERM, F-25000 Besançon, France. Electronic address: marc.pudlo@univ-fcomte.fr.

Classifications MeSH