Ferroquine, an Ingenious Antimalarial Drug –Thoughts on the Mechanism of Action

doi:10.3390/molecules13112900

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Molecules 2008, 13(11), 2900-2907; doi:10.3390/molecules13112900

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Ferroquine, an Ingenious Antimalarial Drug –Thoughts on the Mechanism of Action

Faustine Dubar ¹ , Jamal Khalife ² , Jacques Brocard ¹ , Daniel Dive ² and Christophe Biot ¹^,*

¹ Université des Sciences et Technologies de Lille, Unité de Catalyse et Chimie du Solide – UMR CNRS 8181, Ecole Nationale Supérieure de Chimie de Lille, Bâtiment C7, B.P. 90108, 59652 Villeneuve d' Ascq cedex, France ² Inserm U547, Institut Pasteur, 1 rue du Pr Calmette, B.P. 245, 59019 Lille Cedex, France

* Author to whom correspondence should be addressed.

Received: 22 October 2008; in revised form: 14 November 2008 / Accepted: 18 November 2008 / Published: 20 November 2008

(This article belongs to the Special Issue Neglected Diseases: Medicinal Chemistry and Natural Product Chemistry)

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Abstract: Ferroquine (FQ or SR97193) is a novel antimalarial drug candidate, currently in development at Sanofi-Aventis. In contrast to conventional drugs, FQ is the first organometallic drug: a ferrocenyl group covalently flanked by a 4-aminoquinoline and a basic alkylamine. FQ is able to overcome the CQ resistance problem, an important limit to the control of Plasmodium falciparum, the principal causative agent of malaria. After fifteen years of effort, it is now possible to propose a multifactorial mechanism of action of FQ by its capacity to target lipids, to inhibit the formation of hemozoin and to generate reactive oxygen species.

Keywords: Malaria; Bioorganometallics; Ferroquine; Mechanism of action; Resistance

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MDPI and ACS Style

Dubar, F.; Khalife, J.; Brocard, J.; Dive, D.; Biot, C. Ferroquine, an Ingenious Antimalarial Drug –Thoughts on the Mechanism of Action. Molecules 2008, 13, 2900-2907.

AMA Style

Dubar F., Khalife J., Brocard J., Dive D., Biot C. Ferroquine, an Ingenious Antimalarial Drug –Thoughts on the Mechanism of Action. Molecules. 2008; 13(11):2900-2907.

Chicago/Turabian Style

Dubar, Faustine; Khalife, Jamal; Brocard, Jacques; Dive, Daniel; Biot, Christophe. 2008. "Ferroquine, an Ingenious Antimalarial Drug –Thoughts on the Mechanism of Action." Molecules 13, no. 11: 2900-2907.

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