Article Dans Une Revue Organic & Biomolecular Chemistry Année : 2024

Dynamic covalent bonding (DCB): the bond lability of alkoxyamines as drugs against Schistosoma mansoni and Plasmodium falciparum

Ange W Embo-Ibouanga
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Gérard Audran
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Sylvain R A Marque

Résumé

Dynamic covalent bonding (DCB) has been a rising concept for the past several years in materials sciences. This article describes how the bond lability involved in DCB is applied to develop drugs against tropical parasitic diseases such as malaria and bilharziasis. Recently, we showed that some alkoxyamines (typical molecules exhibiting DCB) exhibit in vitro activities against S. mansoni (for A8L, 100% worm mortality in 48 hours at 10 μgml−1) and P. falciparum (for A8L,IC50 = 270 nM). Here, the combination of enzymatic-physical (solvent effect) activation or of enzymatic-chemical (acetal hydrolysis) activation is used to develop alkoxyamines that show activity against both parasites. The enzymatic step controls the specificity of the drug.
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mardi 3 juin 2025
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Dates et versions

hal-04903248 , version 1 (21-01-2025)

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Ange W Embo-Ibouanga, Michel Nguyen, Lucie Paloque, Jean-Patrick Joly, Raphaël Bikanga, et al.. Dynamic covalent bonding (DCB): the bond lability of alkoxyamines as drugs against Schistosoma mansoni and Plasmodium falciparum. Organic & Biomolecular Chemistry, 2024, 23 (3), pp.734-743. ⟨10.1039/D4OB01644K⟩. ⟨hal-04903248⟩
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