Sabine Fletcher

TL;DR: One chemical subseries was found to exhibit oral activity but contained a labile ester that could not be replaced without loss of activity, and the original hit exhibited remarkable sensitivity to minor structural change.

TL;DR: A high-throughput screening campaign using a prefractionated natural product library and an in vitro antimalarial assay identified active fractions derived from the Australian marine sponge Plakortis lita as thiaplakortones A-D, the most active natural product.

TL;DR: The design, synthesis, and evaluation of a series of hydroxamic acid-based inhibitors capable of potent inhibition of both Plasmodium falciparum aminopeptidases activity and parasite growth in culture are described and demonstrated.

TL;DR: A novel high throughput approach for the identification of chemically diverse inhibitors of the CoA synthesis pathway is reported, substantiates the suitability of this approach to identify novel starting points for future anti-malarial drug development.

TL;DR: The disubstituted triazine dimer 6k represents a new class of orally available antimalarial compounds of considerable interest for further development and has high in vitro potency against P. falciparum lines resistant to chloroquine and artemisinin.