Identification of nuclear proteins that differentially interact with <em>Plasmodium falciparum</em> var gene promoters (Publications)
variation and cytoadherence of infected erythrocytes in malaria. Approximately 50 var genes per parasite genome code for this highly polymorphic surface protein. We showed recently that chromosome-central
<em>In vitro</em> efficacy of dicationic compounds and mefloquine enantiomers against <em>Echinococcus multilocularis</em> metacestodes (Publications)
recently validated assay based on the release of functional phosphoglucose isomerase (PGI) from dying parasites, the activities of 26 dicationic compounds and of the (+)- and (-)-erythro-enantiomers of mefloquine
Antiprotozoal activity of 1-phenethyl-4-aminopiperidine derivatives (Publications)
A series of 44 4-aminopiperidine derivatives was screened in vitro against four protozoan parasites (Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, and Plasmodium falciparum).
Community effectiveness of intermittent preventive treatment for infants (IPTi) in rural southern Tanzania (Publications)
comparison areas (P = 0.06). In a "per protocol" analysis of children who had recently received IPTi, parasite prevalence was 22%, 19 percentage points lower than comparison children (P = 0.01). IPTi can be
Antikinetoplastid antimitotic activity and metabolic stability of dinitroaniline sulfonamides and benzamides (Publications)
N(4)-di-n-butylsulfanilamide (2) show potent in vitro antimitotic activity against kinetoplastid parasites but display poor in vivo activity. Seventeen new dinitroaniline sulfonamide and eleven new benzamide
Synthesis and structure-activity analysis of new phosphonium salts with potent activity against African trypanosomes (Publications)
and TbB48). More than half of the compounds tested showed a submicromolar EC(50) against these parasites. The compounds did not display any cross-resistance to existing diamidine therapies, such as pentamidine
<em>Hippeastrum reticulatum </em>(Amaryllidaceae): alkaloid profiling, biological activities and molecular docking (Publications)
(6alpha-hydroxymaritidine and 6beta-hydroxymaritidine) showed low activity against all protozoan parasites tested and weak AChE-inhibitory activity. Finally, a molecular docking analysis of AChE and BuChE
TKK130 is a 3-hydroxy-propanamidine (HPA) with potent antimalarial <em>in vivo</em> activity and a high barrier to resistance (Publications)
strains. Moreover, in various human cell lines, the compound shows no cytotoxicity and excellent parasite selectivity. The compound inhibits synthetic hemozoin (β-hematin) formation, with IC(50) values
Repurposing a library of human cathepsin L ligands: identification of macrocyclic lactams as potent rhodesain and <em>trypanosoma brucei... (Publications)
Rhodesain (RD) is a parasitic, human cathepsin L (hCatL) like cysteine protease produced by Trypanosoma brucei ( T. b.) species and a potential drug target for the treatment of human African trypanosomiasis
Lead optimization of a pyrrole-based dihydroorotate dehydrogenase inhibitor series for the treatment of malaria (Publications)
target-based DHODH screen. Compounds with nanomolar potency versus Plasmodium DHODH and Plasmodium parasites were identified with good pharmacological properties. X-ray studies showed that the pyrroles bind
