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

Authors :
Douglas J. Minick
Lourdes Rueda
Santiago Ferrer
Pablo Castañeda
Francisco J. Gamo
J. Vidal
María J. Chaparro
Raquel Gabarró
María Santos Martínez
Angel Santos-Villarejo
Jose M. Coteron
Mercedes García
María Belén Jiménez-Díaz
Michael J Witty
Félix Calderón
Sara Prats
Iñigo Angulo-Barturen
Maria Jose Lafuente
Margarita Puente
Jeremy N. Burrows
Gonzalo Colmenarejo
María Luisa León
Nicholas Cammack
Jose M. Bueno
Laura Fernández de las Heras
Esther Fernández
Elena Sandoval
Source :
ACS Medicinal Chemistry Letters. 5:657-661
Publication Year :
2014
Publisher :
American Chemical Society (ACS), 2014.

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.

Details

ISSN :
19485875
Volume :
5
Database :
OpenAIRE
Journal :
ACS Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....ea14a99c5446b043ddbd69925e99aec4
Full Text :
https://doi.org/10.1021/ml500015r