title: Identification and In-Vitro ADME Assessment of a Series of Novel Anti-Malarial Agents Suitable for Hit-to-Lead Chemistry.
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.
authors.affiliation: iThemba Pharmaceuticals , P.O. Box 21, Modderfontein 1645, South Africa.
authors.forename: Chris D
authors.initials: CD
authors.lastname: Edlin
authors.affiliation: iThemba Pharmaceuticals , P.O. Box 21, Modderfontein 1645, South Africa.
authors.forename: Garreth
authors.initials: G
authors.lastname: Morgans
authors.affiliation: iThemba Pharmaceuticals , P.O. Box 21, Modderfontein 1645, South Africa.
authors.forename: Susan
authors.initials: S
authors.lastname: Winks
authors.affiliation: Discovery Biology Institute, Griffith University , Brisbane, Queensland 4111, Australia.
authors.forename: Sandra
authors.initials: S
authors.lastname: Duffy
authors.affiliation: Discovery Biology Institute, Griffith University , Brisbane, Queensland 4111, Australia.
authors.forename: Vicky M
authors.initials: VM
authors.lastname: Avery
authors.affiliation: Swiss Tropical and Public Health Institute , Socinstrasse 57, 4002 Basel, Switzerland.
authors.forename: Sergio
authors.initials: S
authors.lastname: Wittlin
authors.affiliation: Medicines for Malaria Venture , ICCRoute de Pre-Bois 20, P.O. Box 1826, 1215 Geneva, Switzerland.
authors.forename: David
authors.initials: D
authors.lastname: Waterson
authors.affiliation: Medicines for Malaria Venture , ICCRoute de Pre-Bois 20, P.O. Box 1826, 1215 Geneva, Switzerland.
authors.forename: Jeremy
authors.initials: J
authors.lastname: Burrows
authors.affiliation: Medical Research Council Technology , 1-3 Burtonhole Lane, Mill Hill, London, United Kingdom.
authors.forename: Justin
authors.initials: J
authors.lastname: Bryans
keywords: Plasmodium falciparum; Screening; hit-to-lead chemistry; phenotypic screening