Design, synthesis and biological evalutation of new antiplasmodialcompounds related to ellagic acid

Ellagic acid is a polyphenol abundantly found in plants and ishighly concentrated in common fruits such as raspberries, strawberries, pomegranate. This compound possesses a wide range of biological activities, suggesting beneficial effects on human health. Taking into account its high antiplasmodial activity both in vitro and in vivo (after intraperitoneal injection) and considering its low bioavailability (linked to limited water solubility), we envisage the design of original prodrugs and derivatives showing improved pharmacokinetic parameters (and potentiallyimproved antiplasmodial activity). After in vitro evaluation of their activity on Plasmodium sp. and on recombinant cysteine protease and assessment of the safety on an in vitro cytotoxic assay, the lead compounds will be investigated for their antiplasmodial activity in vivo. These new compounds should constitute a set of powerful drug candidates for the treatment of malaria and should help refining the knowledge of the mechanism of action of this class of compounds.

Drug-based Strategies

Oct 2017 — Dec 2019

Belgium