Screening the Pathogen Box to Discover and Characterize New Cruzain and CatL Inhibitors.

Chagas disease and Human African Trypanosomiasis, caused by and , respectively, pose relevant health challenges throughout the world, placing 65 to 70 million people at risk each. Given the limited efficacy and severe side effects associated with current chemotherapy, new drugs are urgently needed for both diseases. Here, we report the screening of the Pathogen Box collection against cruzain and CatL, validated targets for Chagas disease and Human African Trypanosomiasis, respectively.

Synthesis, Design, and Structure-Activity Relationship of a Benzenesulfonylpiperazine Series against Trypanosoma cruzi.

Chagas disease is a neglected tropical disease, endemic in Latin America and caused by the protozoan parasite Trypanosoma cruzi. Available treatments show low cure efficacy during the chronic phase of the disease and cause a series of side effects, reinforcing the need to develop new drugs against Chagas disease. In this work, we describe the optimization of a trypanocidal hit compound recently reported in phenotypic high-throughput screening studies against Trypanosoma cruzi.