Antiparasitic activity of Squaramides

The present invention provides a series of squaramide-based compounds as antiparasitic agents for the treatment of leishmaniasis and Chagas disease in particular.

For the preparation of a medicinal product for the treatment and/or prevention of parasite diseases.



The therapeutic agents developed to date are based on nitrogen-containing heterocycles such as nitrofuran (nifurtimox) or nitroimidazole derivatives (benznidazole). Both nifurtimox and benznidazole are only effective against the acute phase of the disease and have very limited efficacy against the chronic phase. They are also very toxic and cause severe side-effects such as pancreatitis and cardiac toxicity.


Pentavalent antimony derivatives such as sodium stibogluconate (Pentostam) or meglumine antimoniate (Glucantime) have been used to treat leishmaniasis for more than 70 years. Other medicinal products used include amphotericin B (AmBiosomeR), which is administered for up to 10 days and is non-toxic but very expensive ($1500-2400 per treatment), miltefosine, which is administered orally but treatment lasts for 4 weeks and its use is restricted in pregnant women and children, pentamidine and ketoconazole. 


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