Investigation of the Redox Behavior of Ferroquine, a New Antimalarial

Chavain, Natascha; Vezin, Herve; Dive, Daniel; Touati, Nadia; Paul, Jean-Francois; Buisine, Eric; Biot, Christophe

Document type :

Article dans une revue scientifique

DOI :

10.1021/mp800007x

Permalink :

http://hdl.handle.net/20.500.12210/55867

Title :

Investigation of the Redox Behavior of Ferroquine, a New Antimalarial

Author(s) :

Chavain, Natascha [Auteur]
Unité de Catalyse et Chimie du Solide - UMR 8181 [UCCS]
Vezin, Herve [Auteur]

Laboratoire de Chimie Organique et Macromoleculaire [UMR CNRS 8009]
Dive, Daniel [Auteur]
Centre d’Infection et d’Immunité de Lille - INSERM U 1019 - UMR 9017 - UMR 8204 [CIIL]
Touati, Nadia [Auteur]
Laboratoire de Chimie Organique et Macromoleculaire [UMR CNRS 8009]
Paul, Jean-Francois [Auteur]

Unité de Catalyse et Chimie du Solide - UMR 8181 [UCCS]
Buisine, Eric [Auteur]
Laboratoire de Chimie Organique et Macromoleculaire [UMR CNRS 8009]
Biot, Christophe [Auteur]

Unité de Catalyse et Chimie du Solide - UMR 8181 [UCCS]

Journal title :

Molecular pharmaceutics

Pages :

710-716

Publisher :

American Chemical Society

Publication date :

2008-06-19

ISSN :

1543-8384

English keyword(s) :

Hydroxyls
Redox reactions
Parasites
Sandwich compounds
Quantum mechanics

HAL domain(s) :

Chimie/Chimie théorique et/ou physique

English abstract : [en]

Ferroquine (FQ or SR97193) is a unique ferrocene antimalarial drug candidate which just entered phase IIb clinical trials in autumn 2007. FQ is able to overcome the chloroquine (CQ) resistance problem, an important limit ...
Show more >Ferroquine (FQ or SR97193) is a unique ferrocene antimalarial drug candidate which just entered phase IIb clinical trials in autumn 2007. FQ is able to overcome the chloroquine (CQ) resistance problem, an important limit to the control of Plasmodium falciparum, the principal causative agent of malaria. However, as for other therapeutic agents such as chloroquine (CQ) and artemisin, its mechanism of action remains partially unknown. Most investigations have so far focused on comparing the activity of FQ to that of CQ in order to understand how the ferrocene core contributes to a stronger antiplasmodial activity. Studies have already shown that the ferrocene altered the shape, volume, lipophilicity, basicity and also electronic profile of the parent molecule and, hence, its pharmacodynamic behavior. However, few investigations have been undertaken to probe the real contribution of redox properties of the ferrocene (iron(II))/ferricinium (iron(III)) system in FQ as reported in this article. In our experimental and theoretical approach, we considered the redox profile of the ferrocene core of FQ in the specific conditions (acidic and oxidizing) of the parasitic digestive vacuole as a possible discriminating property from CQ in the antimalarial activity.Show less >

Language :

Anglais

Audience :

Internationale

Popular science :

Non

Collections :

Centre d'Infection et d'Immunité de Lille (CIIL) - U1019 - UMR 9017

Source :

Harvested from HAL

Submission date :

2021-10-10T01:30:44Z

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