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Purification of Extracellular Trypanosomes, Including African, from Blood by Anion-Exchangers (Diethylaminoethyl-cellulose Columns)
Published on: April 6, 2019
Diamine and aminoalcohol derivatives active against Trypanosoma brucei
Esther Del Olmo1, Rosario Diaz-González, Ricardo Escarcena
1Departamento de Química Farmacéutica, Facultad de Farmacia - CIETUS, Universidad de Salamanca, Campus Unamuno, E-37007 Salamanca, Spain. olmo@usal.es
Abstract:
Twenty compounds selected as representative members of three series of long-chain 1,2-diamines, 2-amino-1-alkanols and 1-amino-2-alkanols structurally related to dihydrosphingosin, were synthesized and tested in vitro for their ability to inhibit the sleeping sickness parasites Trypanosoma bruceirhodesiense and Trypanosoma brucei gambiense. Eight compounds showed EC(50) values in the submicromolar range, with selectivity indexes up to 39 related to the respective cytotoxicity values for Vero cells. The parasite phenotype detected after treatment with the most potent compounds showed irreversible cell morphology alterations of the flagellar pocket that lead to inhibition of cell growth and parasite death.
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