Molecules
(Jun 2015)
Trypanocidal Activity of Long Chain Diamines and Aminoalcohols
Ana L. Legarda-Ceballos,
Esther del Olmo,
Julio López-Abán,
Ricardo Escarcena,
Luis A. Bustos,
Cristina Fonseca-Berzal,
Alicia Gómez-Barrio,
Juan C. Dib,
Arturo San Feliciano,
Antonio Muro
Affiliations
Ana L. Legarda-Ceballos
Laboratory of Molecular Immunology and Parasitology, Faculty of Pharmacy, CIETUS, IBSAL, Universidad de Salamanca, 37007-Salamanca, Spain
Esther del Olmo
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, CIETUS, IBSAL, Universidad de Salamanca, 37007-Salamanca, Spain
Julio López-Abán
Laboratory of Molecular Immunology and Parasitology, Faculty of Pharmacy, CIETUS, IBSAL, Universidad de Salamanca, 37007-Salamanca, Spain
Ricardo Escarcena
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, CIETUS, IBSAL, Universidad de Salamanca, 37007-Salamanca, Spain
Luis A. Bustos
Department of Pharmaceutical Sciences, Faculty of Sciences, Catholic University of the North, 0610-Antofagasta, Chile
Cristina Fonseca-Berzal
Department of Parasitology, Faculty of Pharmacy, Complutense University of Madrid (CEI Campus Moncloa, UCM-UPM & CSIC), 28040-Madrid, Spain
Alicia Gómez-Barrio
Department of Parasitology, Faculty of Pharmacy, Complutense University of Madrid (CEI Campus Moncloa, UCM-UPM & CSIC), 28040-Madrid, Spain
Juan C. Dib
Research Center on Health for the Tropics, (CIST), Carretera Troncal del Caribe, Sector Mamatoco, Santa Marta, Magdalena, Colombia
Arturo San Feliciano
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, CIETUS, IBSAL, Universidad de Salamanca, 37007-Salamanca, Spain
Antonio Muro
Laboratory of Molecular Immunology and Parasitology, Faculty of Pharmacy, CIETUS, IBSAL, Universidad de Salamanca, 37007-Salamanca, Spain
DOI
https://doi.org/10.3390/molecules200611554
Journal volume & issue
Vol. 20,
no. 6
pp.
11554
– 11568
Abstract
Read online
Thirteen aminoalcohols and eight diamines were obtained and tested against Trypanosoma cruzi epimastigotes strains MG, JEM and CL-B5 clone. Some of them were equal or more potent (1.0–6.6 times) than the reference compound nifurtimox. From them, three aminoalcohols and two diamines were selected for amastigotes assays. Compound 5 was as potent as the reference drug nifurtimox against amastigotes of the CL-B5 strain (IC50 = 0.6 µM), with a selectivity index of 54.
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