11 research outputs found

    Denovo generated human red blood cells in humanized mice support Plasmodium falciparum infection

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    10.1371/journal.pone.0129825PLoS ONE106e012982

    Antibodies targeting the PfRH1 binding domain inhibit invasion of Plasmodium falciparum merozoites

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    10.1371/journal.ppat.1000104PLoS Pathogens47e100010

    Synthesis, characterization and in vitro evaluation of novel enantiomerically-pure sulphonamide antimalarials

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    Malaria parasites are currently gaining drug-resistance rapidly, across countries and continents. Hence, the discovery and development of novel chemical scaffolds, with superior antimalarial activity remain an important priority, for the developing world. Our report describes the development, characterization and evaluation of novel bepotastine-based sulphonamide antimalarials inhibiting asexual stage development of Plasmodium falciparum parasites in vitro. The screening results showed potent inhibitory activity of a number of novel sulphonamides against P. falciparum at low micromolar concentrations, in particular in late-stage parasite development. Based on computational studies we hypothesize N-myristoyltransferase as the target of the compounds developed here. Our results demonstrate the value of novel bepotastine-based sulphonamide compounds for targeting the asexual developmental stages of P. falciparum. © 2015 The Royal Society of Chemistry
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