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

  • ACS Med Chem Lett. 2014 Mar 26;5(6):657-61. doi: 10.1021/ml500015r.
María J Chaparro  1 ,  Jaume Vidal  1 ,  Iñigo Angulo-Barturen  1 ,  José M Bueno  1 ,  Jeremy Burrows  2 ,  Nicholas Cammack  1 ,  Pablo Castañeda  1 ,  Gonzalo Colmenarejo  3 ,  José M Coterón  1 ,  Laura de Las Heras  1 ,  Esther Fernández  1 ,  Santiago Ferrer  1 ,  Raquel Gabarró  1 ,  Francisco J Gamo  1 ,  Mercedes García  1 ,  María B Jiménez-Díaz  1 ,  María J Lafuente  1 ,  María L León  1 ,  María S Martínez  1 ,  Douglas Minick  4 ,  Sara Prats  1 ,  Margarita Puente  1 ,  Lourdes Rueda  1 ,  Elena Sandoval  1 ,  Angel Santos-Villarejo  1 ,  Michael Witty  2 ,  Félix Calderón  1
Affiliations
  • 1. Tres Cantos, Medicines Development Campus, DDW, GlaxoSmithKline , Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain.
  • 2. Medicines for Malaria Venture (MMV) , 20 route de Pré-Bois, 1215 Geneva 15, Switzerland.
  • 3. Centro de Investigación Básica, GlaxoSmithKline , Santiago Grisolía, 28760 Tres Cantos, Madrid, Spain.
  • 4. GlaxoSmithKline , 5 Moore Drive, Research Triangle Park, Durham, North Carolina 27709, United States.
PMID: 24944739 DOI: 10.1021/ml500015r
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.

Keywords
Aminoalcoholes; TCAMS; malaria; mefloquine; tres cantos antimalarial set.
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