Effects of amidine derivatives on parasite-macrophage interaction and evaluation of toxicity.
In this work, the effect of amidine derivatives (with bromine and methoxy as substituents) in the "in vitro" parasite-macrophage interaction was evaluated. The potential toxicity was also analyzed. The results show that the methoxy-derivative was able to decrease the percentage of "in vitro" infection, being not hazardous to the host cell. Furthermore, experiments using Balb/c mice showed that this compound was very effective in avoiding infection in these animals. On the other hand, the compound with bromine as substituent was toxic to macrophages and unable to prevent infection in Balb/c mice. Pentamidine isethionate, used as reference drug, was not efficient in both experiments.
Department of Immunology, Oswaldo Cruz Institute, Oswaldo Cruz Foundation (FIOCRUZ), Rio de Janeiro, Brazil.
Rosane M
RM
Temporal
Léa
L
Cysne-Finkelstein
Aurea
A
Echevarria
Marco A S
MA
de Souza
Mônica
M
Sertà
Antônio J
AJ
da Silva-Gonçalves
Claude
C
Pirmez
Lenor L
LL
Leon
D000578:Amidines / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity*; D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity*; D066298:In Vitro Techniques; D007894:Leishmania mexicana / Q000187:drug effects*; D007928:Lethal Dose 50; D017737:Macrophages, Peritoneal / Q000187:drug effects* / Q000469:parasitology*; D051379:Mice; D008807:Mice, Inbred BALB C; D013329:Structure-Activity Relationship
D000578:Amidines; D000981:Antiprotozoal Agents