Reference : Potential of caffeic acid derivatives as antimalarial leads.
Scientific journals : Article
Human health sciences : Pharmacy, pharmacology & toxicology
http://hdl.handle.net/2268/267072
Potential of caffeic acid derivatives as antimalarial leads.
English
Degotte, Gilles mailto [Université de Liège - ULiège > Département de pharmacie > Pharmacognosie >]
Pirotte, Bernard mailto [Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique >]
Francotte, Pierre mailto [Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique >]
Frederich, Michel mailto [Université de Liège - ULiège > Département de pharmacie > Pharmacognosie >]
In press
Letters in Drug Design and Discovery
Bentham Science Publishers
Yes (verified by ORBi)
International
1570-1808
United Arab Emirates
[en] malaria ; caffeic acid ; Plasmodium ; organic synthesis
[en] Malaria remains one of the deadliest infectious disease in 2021. Indeed, this infection, mostly caused by a protozoon called Plasmodium falciparum, is responsible annually for more than 200 million cases and around 400 000 related deaths, mainly in Africa. Despite the availability of efficient drugs, we observe an increase of patients since 2015, which could find its origin in development of resistances from the parasite but also from its vectors, Anopheles mosquitoes. Consequently, it is necessary to search for new alternative treatments. Polyphenols, and more precisely small phenolic acids, could represent a good starting point for new antimalarials. Indeed, these molecules, such as caffeic acid (1), exhibit several pharmacological activities and an interesting pharmacokinetic profile. Therefore, we have developed several small derivatives of this scaffold to define the potential pharmacophore responsible for the antiplasmodial properties. We have obtained a good to low activity on Plasmodium (IC50 = 16-241 µM) with selectivity against human cells, especially for small esters (2-6, SI > 3). These structures have highlighted the need of catechol and carboxyl moieties in the anti-Plasmodium effect. Unfortunately, none of them seemed sufficiently effective to become a new antimalarial, but they could be new leads for future development.
Centre Interdisciplinaire de Recherche sur le Médicament - CIRM
Fonds de la Recherche Scientifique - F.R.S.-FNRS ; Fonds Léon Fredericq
Malagic
Researchers
http://hdl.handle.net/2268/267072

File(s) associated to this reference

Fulltext file(s):

FileCommentaryVersionSizeAccess
Restricted access
DEGOTTE_Article.pdfAuthor preprint448.32 kBRequest copy

Bookmark and Share SFX Query

All documents in ORBi are protected by a user license.