Abstract
There is an urgent need for the development of new antimalarial compounds. As a result of a phenotypic screen, several compounds with potent activity against the parasite Plasmodium falciparum were identified. Characterization of these compounds is discussed, along with approaches to optimise the physicochemical properties. The in vitro antimalarial activity of these compounds against P. falciparum K1 had EC50 values in the range of 0.09–29 μM, and generally good selectivity (typically >100-fold) compared to a mammalian cell line (L6). One example showed no significant activity against a rodent model of malaria, and more work is needed to optimise these compounds.
Highlights
Malaria is a serious endemic disease and is a major threat to public health in more than 100 countries [1,2]
Malaria is caused by protozoan parasites of the species Plasmodium [5], with Plasmodium falciparum being responsible for most malaria-related deaths
We have recently reported the identification of a hit (TDR32750) [6,7] from a screen of the ChemDiv5000 ‘maximally structurally diverse’ compound collection against P. falciparum
Summary
Malaria is a serious endemic disease and is a major threat to public health in more than 100 countries [1,2]. We have recently reported the identification of a hit (TDR32750) [6,7] from a screen of the ChemDiv5000 ‘maximally structurally diverse’ compound collection against P. falciparum. This screen was carried out by the World Health Organisation Programme for Research and Training in Tropical Medicine (Fig. 1). The activity of compounds against the chloroquine and pyrimethamine resistant (K1) strain of P. falciparum is reported, as well as a counter-screen (EC50) against the L6 murine cell line, to provide an indication of selectivity (Table 1, Fig. 2)
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