Human parasitic diseases are the foremost threat to human health and welfare around the world. American trypanosomiasis, or Chagas� disease, is a neglected disease against which the efficacy of currently available drugs ranges from limited to none. Thus, there is an urgent need for new chemotherapeutic agents. Cruzain is the major cysteine protease of Trypanosoma cruzi. This enzyme is relevant to a key biochemical path of the parasite's life-cycle and also to the parasite-host relationship. In this context, cruzain is an attractive target for antitrypanosomal chemotherapy. We tested 20 compounds (9 chalcones and 11 aryl hydrazones) as potential cruzain inhibitors. All derivatives tested were active with 50% inhibitory concentration (IC50) between 3.38 + 0.35 and 12.78 + 3.8 mmol. The compound 4-methyl-N'-(5-nitrothiophen-2-yl)methylene)benzohydrazide showed to be the most active of the series. The structural scaffold of the molecules studied herein suggests a good starting point for the design of new potent inhibitors against cruzain.

Cruzain inhibitory activity of chalcones and hydrazones

239th National Meeting (2010)

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