Substituted 2-phenyl-imidazopyridines: a new class of drug leads for human African trypanosomiasis (Publications)
a substituted 2-(3-aminophenyl)imidazopyridine. This compound showed antiparasitic activity of parasites in vitro with an EC50 of 2 nM and displayed reasonable drug-like properties when tested in a number [...] mice infected with Trypanosoma brucei when dosed orally down to 2.5 mg/kg. Given its potent anti-parasitic properties and its ease of synthesis, compound 87 represents a new lead for the development of drugs
Antiprotozoal screening of 60 south African plants, and the identification of the antitrypanosomal germacranolides schkuhrin I and II (Publications)
extracts which inhibited the growth of one or more parasites with more than 95 % at 10 microg/mL, the IC50 values against all four protozoal parasites and cytotoxic IC50 values against L6 myoblasts were
Characterization of choline uptake in<em> Trypanosoma brucei</em> procyclic and bloodstream forms (Publications)
phospholipids, such as phosphatidylcholine (PC). According to published data, Trypanosoma brucei parasites are unable to take up choline from the environment but instead use lyso-phosphatidylcholine as precursor [...] analogs that have been established as anti-malarials. Together, our results show that T. brucei parasites express an uptake system for choline and that exogenous choline is used for PC synthesis
Strongyloidiasis - the most neglected of the neglected tropical diseases? (Publications)
ic light infections to chronic symptomatic strongyloidiasis. Uncontrolled multiplication of the parasite (hyperinfection) and potentially life-threatening dissemination of larvae to all internal organs [...] could cause serious problems in the community. Therefore, we need to carefully investigate this parasite in order to develop and implement effective control programmes
Exploring a tetrahydroquinoline antimalarial hit from the medicines for malaria pathogen box and the identification of its mode of resistance as... (Publications)
vitro models of malaria and was found to be active against multiple life-cycle stages of Plasmodium parasites. The mode of resistance, and putatively its mode of action, was identified as Plasmodium falciparum [...] of the ribosome along mRNA. The compound maintains activity against a series of drug-resistant parasite strains. The structural motif of the tetrahydroquinoline ( 2 ) was explored in a chemistry program
Identification of 2,4-disubstituted imidazopyridines as hemozoin formation inhibitors with fast-killing kinetics and <em>in vivo</em> efficacy in the... (Publications)
Kinase library, was identified from a high throughput phenotypic screen against the human malaria parasite Plasmodium falciparum. Hit compounds showed moderate asexual blood stage activity. During lead [...] compound 37 showed good exposure in mice combined with good in vitro activity against the malaria parasite, which translated into in vivo efficacy in the P. falciparum NOD-scid IL-2Rgamma(null) (NSG) mouse
Antimalarial benzimidazole derivatives incorporating phenolic mannich base side chains inhibit microtubule and hemozoin formation: structure-activity... (Publications)
which were only active against asexual blood stage (ABS) parasites. Further, the former demonstrated microtubule inhibitory activity in ABS parasites but more significantly in stage II/III gametocytes. In
Real-time and automated monitoring of antischistosomal drug activity profiles for screening of compound libraries (Publications)
initially screening 57 repurposed compounds against larvae, five drugs are identified, which reduce parasite viability by more than 70%. The activity profiles of the selected drugs are then investigated via [...] potency and rapid action, which renders them suitable candidates for follow-up tests against adult parasites. The study shows that our device is a reliable tool for real-time drug screening analysis of libraries
TrypanoCyc: a community-led biochemical pathways database for <em>Trypanosoma brucei</em> (Publications)
which describes the generic and condition-specific metabolic network of Trypanosoma brucei, a parasitic protozoan responsible for human and animal African trypanosomiasis. In addition to enabling navigation [...] MetExplore, yielding a novel environment in which to visualise the metabolism of this important parasite
High levels of genetic diversity of <em>Plasmodium falciparum</em> populations in Papua New Guinea despite variable infection prevalence (Publications)
control. Here, we investigate the relationship between local variation in malaria epidemiology and parasite genetic diversity in Papua New Guinea (PNG). Cross-sectional malaria surveys were performed in 14 [...] In highly endemic areas, differences in infection prevalence may not translate into a decrease in parasite population diversity
