Leishmaniasis is a protozoan parasitic disease that puts 350 million people at risk in 88 countries. It is caused by more than 20 species of the genus Leishmania. We have synthesized and analyzed the anti-leishmanial properties of a set of 2,4-diaminoquinazoline analogues. These compounds have been found to display single digit micromolar or high nanomolar activity against intracellular Leishmania donovani in vitro and also possess selectivity indexes >20 (toxicity against J774 macrophages/activity against intracellular L. donovani), making these compounds interesting leads. One 2,4-diaminoquinazoline in this series, KVH14, also displays efficacy in our murine model of visceral leishmaniasis, reducing liver parasitemia by 36% when given by the intraperitoneal route at 15 mg/kg/day for five consecutive days.

2,4-diaminoquinazolines as anti-leishmanials

243rd National Meeting (2012)

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