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Case Study of Small Molecules As Antimalarials: 2-Amino-1-phenylethanol (APE) Derivatives
María J Chaparro1, Jaume Vidal1, Iñigo Angulo-Barturen1
1Tres Cantos, Medicines Development Campus, DDW, GlaxoSmithKline , Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
Abstract:
Antiparasitic oral drugs have been associated to lipophilic molecules due to their intrinsic permeability. However, these kind of molecules are associated to numerous adverse effects, which have been extensively studied. Within the Tres Cantos Antimalarial Set (TCAMS) we have identified two small, soluble and simple hits that even presenting antiplasmodial activities in the range of 0.4-0.5 μM are able to show in vivo activity.
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