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Last Updated: 31/07/2024
Development of new lead antimalarials targeting parasite coenzyme A biosynthesis and utilisation
Objectives
This project aims to test new lead antimalarials targeting parasite coenzyme A in several biological assays to guide the synthesis of derivatives with improved pharmaceutical profiles, and evaluate the efficacy of the most promising compounds in a mouse model of malaria.
Malaria is a life-threatening disease caused by Plasmodium parasites transmitted to people through the bites of infected female mosquitoes. There were 241 million cases of malaria worldwide in 2020 (~500/year in Canada), leading to 627,000 deaths (a 12% increase compared to 2019). Most of the deaths were children under the age of 5 years. Unfortunately, the effectiveness of current antimalarial drugs is decreasing progressively, a phenomenon known as drug resistance, and the disease is expected to disperse to higher latitudes as earth’s climate warms up, making the discovery of new drugs to treat malaria ever more crucial. New classes of molecules with a novel mechanism of action are particularly desirable to bypass drug resistance. Interestingly, a new class of compounds that can reduce proliferation of the malaria-causing parasites have been identified. These molecules have a unique mechanism of action, are easy to prepare, potent, and typically non-toxic. This project will generate excellent candidates for the development of new antimalarial drugs.
Apr 2023 — Mar 2028
$599,246