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Monoquaternary ammonium derivatives inhibit growth of protozoan parasites |
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| Authors: | Bahamontes-Rosa N Robin A Ambrosio A R Messias-Reason I Beitz E Flitsch S L Kun J F J |
| Institution: | aDepartment of Parasitology, Institute of Tropical Medicine, University of Tübingen, Wilhelmstrasse 27, D-72074 Tübingen, Germany bManchester Interdisciplinary Biocentre, University of Manchester, 131 Princess Street M1 7DN Manchester, United Kingdom cDepartment of Clinical Pathology, Laboratory Immunopathology, Clinical Hospital, Federal University of Parana, Curitiba, Brazil dDepartment of Pharmaceutical Chemistry, University of Kiel, Gutenbergstrasse 76, 24118 Kiel, Germany |
| Abstract: | The phospholipid metabolism of Plasmodium falciparum-infected erythrocytes has been shown to be an effective pharmacological target for novel chemotherapy. Thirty-seven monoquaternary ammonium derivatives analogous to choline were screened for their potential antiprotozoal activity against P. falciparum and Leishmania braziliensis. Twenty-three compounds inhibited chloroquine resistant and sensitive P. falciparum strains with inhibitory concentrations ranging from 0.001 μM to 47 μM. Among the inhibitors were six compounds with nanomolar activity containing at least one ethyl group in the polar head and a hydrophobic alkyl chain with 10 to 14 methylene groups. Four compounds also exhibited in vitro antileishmanial properties in the micromolar range. |
| Keywords: | Plasmodium falciparum Leishmania braziliensis Monoquaternary ammonium Phospholipid metabolism Aquaporin |
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