Article (Scientific journals)
Polyhydroxybenzoic acid derivatives as potential new antimalarial agents
Degotte, Gilles; Pirotte, Bernard; Frederich, Michel et al.
2021In Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft
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Keywords :
Gallic acid; hydroxybenzoic acid; malaria; medicinal chemistry; plasmodium
Abstract :
[en] With more than 200 million cases and 400,000 related deaths, malaria remains one of the deadliest infectious diseases of 2021. Unfortunately, despite the availability of efficient treatments, we have observed an increase in people infected with malaria since 2015 (from 211 million in 2015 to 229 million in 2019). This trend could partially be due to the development of resistance to all the current drugs. Therefore, there is an urgent need for new alternatives. We have, thus, selected common natural scaffolds, polyhydroxybenzoic acids, and synthesized a library of derivatives to better under- stand the structure–activity relationships explaining their antiplasmodial effect. Only gallic acid derivatives showed a noticeable potential for furtherQ3 developments. Indeed, they showed a selective inhibitory effect on Plasmodium (IC50 ~20 μM, SI > 5) often associated with interesting water solubility. Moreover, this has confirmed the critical importance of free phenolic functions (pyrogallol moiety) for the antimalarial effect. Methyl 4-benzoxy-3,5-dihydroxybenzoate (39) has, for the first time, been recognized as a potential lead for future research because of its marked inhibitory activity against Plasmodium falciparum and its significant hydrosolubility (3.72 mM).
Research center :
CIRM - Centre Interdisciplinaire de Recherche sur le Médicament - ULiège
Disciplines :
Pharmacy, pharmacology & toxicology
Author, co-author :
Degotte, Gilles ;  Université de Liège - ULiège > Département de pharmacie > Pharmacognosie
Pirotte, Bernard ;  Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique
Frederich, Michel  ;  Université de Liège - ULiège > Département de pharmacie > Pharmacognosie
Francotte, Pierre  ;  Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique
Language :
English
Title :
Polyhydroxybenzoic acid derivatives as potential new antimalarial agents
Publication date :
04 August 2021
Journal title :
Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft
ISSN :
0376-0367
Publisher :
Verlag Chemie, Germany
Peer reviewed :
Peer reviewed
Name of the research project :
Malagic
Funders :
F.R.S.-FNRS - Fonds de la Recherche Scientifique [BE]
Fondation Léon Fredericq [BE]
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since 23 July 2021

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