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

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An early hit-to-lead optimization process of a novel benzenesulfonylpiperazine series against Trypanosoma cruzi was started. Synthesis, design, biological evaluation, and SAR study were performed, and compounds with good levels of potency (IC50 ∼5 μM), selectivity (>50) and a promising predicted ADMET profile were identified, being candidates for further development towards therapies for Chagas disease.


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. A hit-to-lead process was initiated and a structure-activity relationship against Trypanosoma cruzi was obtained after the synthesis and biological evaluation of 22 new benzenesulfonylpiperazine derivatives. From this structure-activity relationship study, we identified three compounds with a promising predicted ADMET profile and potency comparable to the reference drug benznidazole, which are candidates for further development towards therapies for Chagas disease.

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