Abstract
This paper describes the preparation of N,N'-disubstituted ethylenediamine and imidazolidine derivatives and their in vitro biological activities against Leishmania species. Of the nine synthesized compounds, five displayed a good activity in both L. amazonensis and L. major promastigotes. The compounds 1,2-Bis(p-methoxybenzyl) ethylenediamine (4) and 1,3-Bis(p-methoxybenzyl)imidazolidines (5) showed the best activity on intracellular amastigotes, with IC50 values of 2.0 and 9.4 microgram/mL, respectively. In addition, none of compounds were cytotoxic against mammalian cells. The leishmanicidal activity can be related with inhibition of polyamine synthesis and cellular penetration within biological membranes.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antiprotozoal Agents / chemical synthesis
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Antiprotozoal Agents / chemistry
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Antiprotozoal Agents / pharmacology*
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Cell Survival / drug effects
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Cells, Cultured
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Ethylenediamines / chemical synthesis
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Ethylenediamines / chemistry
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Ethylenediamines / pharmacology*
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Imidazolidines / chemical synthesis
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Imidazolidines / chemistry
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Imidazolidines / pharmacology*
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Leishmania / drug effects
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Leishmania major / drug effects
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Macrophages, Peritoneal / cytology
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Macrophages, Peritoneal / drug effects*
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Macrophages, Peritoneal / parasitology
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Mice
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Mice, Inbred BALB C
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Models, Chemical
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Molecular Structure
Substances
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Antiprotozoal Agents
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Ethylenediamines
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Imidazolidines
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ethylenediamine