Case Study of Small Molecules As Antimalarials: 2‑Amino-1-phenylethanol (APE) Derivatives

Case Study of Small Molecules As Antimalarials: 2‑Amino-1-phenylethanol (APE) Derivatives

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, s...

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Veröffentlicht in:ACS medicinal chemistry letters 2014-06, Vol.5 (6), p.657-661
Hauptverfasser: Chaparro, María J, Vidal, Jaume, Angulo-Barturen, Íñigo, Bueno, José M, Burrows, Jeremy, Cammack, Nicholas, Castañeda, Pablo, Colmenarejo, Gonzalo, Coterón, José M, de las Heras, Laura, Fernández, Esther, Ferrer, Santiago, Gabarró, Raquel, Gamo, Francisco J, García, Mercedes, Jiménez-Díaz, María B, Lafuente, María J, León, María L, Martínez, María S, Minick, Douglas, Prats, Sara, Puente, Margarita, Rueda, Lourdes, Sandoval, Elena, Santos-Villarejo, Ángel, Witty, Michael, Calderón, Félix
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Sprache:eng
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Letter
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Zusammenfassung: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.
ISSN:1948-5875
1948-5875
DOI:10.1021/ml500015r