After cessation of chloroquine, a comprehensive assessment of cognitive and motor function demonstrated persistence of abnormal behavioral outcomes, 10 days after successful eradication of parasites.
In an attempt to establish whether and to what extent activity as antimalarials and embryotoxicity can be divorced, IC50s for activity in Plasmodium falciparum strains and the NOELs for RBCs were compared. From this comparison, arterolane showed a better safety margin than artemisinin.
A targeted series of chalcone and dienone hybrid compounds containing aminoquinoline and nucleoside templates was synthesized and evaluated for in vitro antimalarial activity. The Cu(I)-catalyzed cycloaddition of azides and terminal alkynes was applied as the hybridization strategy.
A public–private partnership has identified a promising new antimalarial compound that is potently effective against a range of Plasmodium species — including some that are resistant to currently used agents — and possesses the pharmacokinetic properties needed to become a viable drug.
We have been investigating plants traditionally used in Brazil to treat malaria and fevers.
Chloroquine (CQ) resistance in P. falciparum is strongly linked to mutations in the gene pfcrt that gives rise to the protein, PfCRT (P. falciparum chloroquine resistance transporter), located in the parasite's digestive vacuole (DV) membrane .
We are interested in the role (if any) played by cyclophilins in parasite killing by cyclosporins.
We have taken a high-throughput approach toward identifying novel antimalarial chemical inhibitors of prioritized drug targets for Plasmodium falciparum, excluding targets which are inhibited by currently used drugs.
A bioorganometallic approach to malaria therapy led to the discovery of ferroquine (FQ, SSR97193). To assess the importance of the electronic properties of the ferrocenyl group, cyclopentadienyltricarbonylrhenium analogues related to FQ, were synthesized.
We report on the discovery of 3-alkylthio-1,2,4-triazine dimers that are potently toxic to Plasmodium falciparum, with single digit nanomolar activity, and up to several thousand-fold lower toxicity to mammalian cells.