Identification and In-Vitro ADME Assessment of a Series of Novel Anti-Malarial Agents Suitable for Hit-to-Lead Chemistry

Triage of a set of antimalaria hit compounds, identified through high throughput screening against the Chloroquine sensitive (3D7) and resistant (Dd2) parasite <i>Plasmodium falciparum</i> strains identified several novel chemotypes suitable for hit-to-lead chemistry investigation. The set was further refined through investigation of their <i>in vitro</i> ADME properties, which identified templates with good potential to be developed further as antimalarial agents. One example was profiled in an <i>in vivo</i> murine <i>Plasmodium berghei</i> model of malaria infection