In vitro activity of dicationic compounds against a North American foxhound isolate of Leishmania infantum

Canine leishmaniasis caused by Leishmania infantum is enzootic in the North American foxhound population. Currently available chemotherapy for canine leishmaniasis is not completely effective and relapses are common in treated dogs. Pentamidine and related aromatic diamidines possess broad spectrum...

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Bibliographic Details
Published in:Veterinary parasitology 2007-04, Vol.145 (3), p.207-216
Main Authors: Rosypal, Alexa C., Hall, James E., Bakunova, Svetlana, Patrick, Donald A., Bakunov, Stanislav, Stephens, Chad E., Kumar, Arvind, Boykin, David W., Tidwell, Richard R.
Format: Article
Language:English
Subjects:
amidines
Animals
Antileishmanial activity
antiprotozoal agents
Antiprotozoal Agents - chemistry
Antiprotozoal Agents - pharmacology
aromatic compounds
Aromatic diamidines
canine leishmaniasis
cations
Cells, Cultured
Dog Diseases - parasitology
Dogs
In vitro
in vitro studies
Inhibitory Concentration 50
Leishmania infantum
Leishmania infantum - immunology
Leishmania infantum - isolation & purification
leishmaniasis
Leishmaniasis, Visceral - parasitology
Leishmaniasis, Visceral - veterinary
medicinal properties
Molecular Structure
Pentamidine
promastigotes
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Summary:Canine leishmaniasis caused by Leishmania infantum is enzootic in the North American foxhound population. Currently available chemotherapy for canine leishmaniasis is not completely effective and relapses are common in treated dogs. Pentamidine and related aromatic diamidines possess broad spectrum antiprotozoal activity. The in vitro antileishmanial activities of 35 aromatic cationic molecules were determined, using pentamidine as the reference drug. The compounds were examined for activity against promastigotes of L. infantum isolated from a foxhound from Virginia. The compounds most active against Leishmania parasites were reversed amidines. Compound 9, a reversed amidine, exhibited the highest activity against L. infantum, with a 50% inhibitory concentration (IC 50) of 0.0042 μM compared with 14.2 μM for pentamidine. Antileishmanial activities of nine compounds were at least 1000-fold higher relative to the reference drug. Results from this study indicate that several pentamidine-related compounds warrant further investigation as possible new agents for the treatment of canine leishmaniasis.
ISSN:0304-4017
1873-2550
DOI:10.1016/j.vetpar.2007.01.005