New developments in redox chemical delivery systems by means of 1,4-dihydroquinoline-based targetor: Application to galantamine delivery to the brain - ANR - Agence nationale de la recherche Accéder directement au contenu
Article Dans Une Revue European Journal of Medicinal Chemistry Année : 2014

New developments in redox chemical delivery systems by means of 1,4-dihydroquinoline-based targetor: Application to galantamine delivery to the brain

Résumé

The therapeutic efficiency of palliative treatments of AD, mostly based on acetylcholinesterase (AChE) inhibitors, is marred by serious adverse effects due to peripheral activity of these AChE inhibitors. In the literature, a redox-based chemical delivery system (CDS) has been developed to enhance drugs distribution to the brain while reducing peripheral side effects. Herein, we disclose two new synthetic strategies for the preparation of 1,4-dihydroquinoline/quinolinium salt redox-based systems particularly well designed for brain delivery of drugs sensitive to alkylation reactions. These strategies have been applied in the present case to the AChE inhibitor galantamine with the aim of alleviating adverse effects observed with cholinergic AD treatment. The first strategy is based on an intramolecular alkylation reaction as key step, whilst the second strategy relies on a useful coupling between galantamine and quinolinium salt key intermediate. In the course of this work, polymer-supported reagents and a solidphase synthesis approach revealed to be highly helpful to develop this redox-based galantamine CDS.
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Origine : Publication financée par une institution

Dates et versions

hal-03856118 , version 1 (16-11-2022)

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Mihaela-Liliana Tîntas, Lénaïg Foucout, Sylvain Petit, Sylvain Oudeyer, Fabienne Gourand, et al.. New developments in redox chemical delivery systems by means of 1,4-dihydroquinoline-based targetor: Application to galantamine delivery to the brain. European Journal of Medicinal Chemistry, 2014, 81, pp.218 - 226. ⟨10.1016/j.ejmech.2014.05.022⟩. ⟨hal-03856118⟩
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