Identification and In-Vitro ADME Assessment of a Series of Novel Anti-Malarial Agents Suitable for Hit-to-Lead Chemistry
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Morgans, Garreth
Winks, Susan
Duffy, Sandra
Avery, Vicky M
Wittlin, Sergio
Waterson, David
Burrows, Jeremy
Bryans, Justin
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Abstract
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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ACS Medicinal Chemistry Letters
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3
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Medicinal and biomolecular chemistry
Medicinal and biomolecular chemistry not elsewhere classified
Organic chemistry
Organic chemistry not elsewhere classified
Pharmacology and pharmaceutical sciences