Identification and In-Vitro ADME Assessment of a Series of Novel Anti-Malarial Agents Suitable for Hit-to-Lead Chemistry.
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ABSTRACT:
SUBMITTER: Edlin CD
PROVIDER: S-EPMC4025777 | biostudies-literature | 2012 Jul
REPOSITORIES: biostudies-literature
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Identification and In-Vitro ADME Assessment of a Series of Novel Anti-Malarial Agents Suitable for Hit-to-Lead Chemistry.
Edlin Chris D CD Morgans Garreth G Winks Susan S Duffy Sandra S Avery Vicky M VM Wittlin Sergio S Waterson David D Burrows Jeremy J Bryans Justin J
ACS medicinal chemistry letters 20120528 7
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 murin ...[more]
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