Design and Synthesis of Hydroxyferroquine Derivatives with Antimalarial and Antiviral Activities

Christophe Biot (1) , Wassim Daher (2) , Natascha Chavain (1) , Thierry Fandeur (3) , Jamal Khalife (2) , Daniel Dive (2) , Erik de Clercq (4)

1 UCCS - Unité de Catalyse et Chimie du Solide - UMR 8181
2 Schistosomiase, paludisme et inflammation
3 TOURS UMR IMMUNOLOGIE PARASIT - Immunologie parasitaire
4 Rega Institute for Medical Research [Leuven, België]

Three ferroquine (FQ) derivatives, closely mimicking the antimalarial drug hydroxychloroquine (HCQ), have been prepared. Whereas these organometallic compounds provide the expected reduced cytotoxic effects compared to FQ, they inhibit in vitro growth of Plasmodium falciparum far better than chloroquine (CQ). Moreover, this new class of bioorganometallic compounds exert antiviral effects with some selectivity toward SARS-CoV infection. These new drugs may offer an interesting alternative for Asia where SARS originated and malaria has remained endemic.

Domaines: Chimie thérapeutique

Christophe Biot, Wassim Daher, Natascha Chavain, Thierry Fandeur, Jamal Khalife, et al.. Design and Synthesis of Hydroxyferroquine Derivatives with Antimalarial and Antiviral Activities. Journal of Medicinal Chemistry, 2006, 49, pp.2845. ⟨10.1021/jm0601856⟩. ⟨hal-00099876⟩