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Updated: Jun 3, 2026

In Vitro Drug Screening Against All Life Cycle Stages of Trypanosoma cruzi Using Parasites Expressing β-galactosidase
Published on: November 5, 2021
Synthesis and anti-Trypanosoma cruzi activity of β-lapachone analogues
Sabrina Baptista Ferreira1, Kelly Salomão, Fernando de Carvalho da Silva
1Departamento de Química Orgânica, Instituto de Química, UFRJ, 21949-900 Rio de Janeiro, RJ, Brazil.
Abstract:
The available chemotherapy for Chagas disease, caused by Trypanosoma cruzi, is unsatisfactory; therefore, there is an intense effort to find new drugs for the treatment of this disease. In our laboratory, we have analyzed the effect on bloodstream trypomastigotes of 16 new naphthoquinone analogues of β-lapachone modified in the pyran ring, aiming to find a new prototype with high trypanocidal activity. The new compounds presented a broad spectrum of activity, and five of them presented IC(50)/24 h in the range of 22-63 μM, whereas β-lapachone had a higher value of 391.5 ± 16.5 μM.
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