BioCentury
ARTICLE | Distillery Therapeutics

Therapeutics: An undetermined target

December 10, 2015 8:00 AM UTC

In vitro and hamster studies identified aminopyrazole ureas that could help treat visceral leishmaniasis. Chemical synthesis and testing of aminopyrazole urea analogs in Leishmania infantum-infected mouse macrophages identified several compounds that inhibited growth of intracellular amastigotes with IC50 values of 0.064-2.11 μM. In an L. infantum-infected hamster model of visceral leishmaniasis, one compound decreased parasite burden in liver and spleen compared with vehicle and with potency comparable to Impavido miltefosine (92.7% and 97.8% in liver and 95% and 99.6% in spleen, respectively). Next steps could include optimization of the most potent compounds...