Ange W Embo-Ibouanga, Michel Nguyen, Lucie Paloque, Jean-Patrick Joly, Raphaël Bikanga, Jean-Michel Augereau, Anne Robert, Gérard Audran, Philippe Mellet, Jérôme Boissier, Françoise Benoit-Vical, Sylvain R A Marque
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Abstract
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 μg ml-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.
期刊介绍：
Organic & Biomolecular Chemistry is an international journal using integrated research in chemistry-organic chemistry. Founded in 2003 by the Royal Society of Chemistry, the journal is published in Semimonthly issues and has been indexed by SCIE, a leading international database. The journal focuses on the key research and cutting-edge progress in the field of chemistry-organic chemistry, publishes and reports the research results in this field in a timely manner, and is committed to becoming a window and platform for rapid academic exchanges among peers in this field. The journal's impact factor in 2023 is 2.9, and its CiteScore is 5.5.
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