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

28 May 2012

Chris D. Edlin, Garreth Morgans, Susan Winks, Sandra Duffy, Vicky M. Avery, Sergio Wittlin, David Waterson, Jeremy Burrows, and Justin Bryans

ACS Medicinal Chemistry Letters
DOI: 10.1021/ml300091c

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

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