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Arzneimittelforschung ; 52(6): 489-93, 2002.
Article in English | MEDLINE | ID: mdl-12109051

ABSTRACT

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.


Subject(s)
Amidines/pharmacology , Amidines/toxicity , Antiprotozoal Agents/pharmacology , Antiprotozoal Agents/toxicity , Leishmania mexicana/drug effects , Macrophages, Peritoneal/drug effects , Macrophages, Peritoneal/parasitology , Amidines/chemistry , Animals , Antiprotozoal Agents/chemistry , In Vitro Techniques , Lethal Dose 50 , Mice , Mice, Inbred BALB C , Structure-Activity Relationship
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