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Antiprotozoal Agents

Antiprotozoal Agents

Leishmaniasis is a widespread parasitic disease caused by several Leishmania species. It affects millions of people each year and remains a major public health problem in endemic regions. First-line treatment relies on pentavalent antimonials, including meglumine antimoniate and sodium stibogluconate. Even so, how these drugs work has not been fully clear, especially their interaction with parasite-specific biochemical pathways. One key target is trypanothione reductase (TR), an enzyme that...

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Updated: Jun 14, 2026

RNA Catalyst as a Reporter for Screening Drugs against RNA Editing in Trypanosomes

RNA Catalyst as a Reporter for Screening Drugs against RNA Editing in Trypanosomes

Published on: July 22, 2014

An In Silico and In Vitro Approach Identified Potential Trypanothione Synthetase Inhibitors with Trypanocidal

Rogelio Gómez-Escobedo¹, Domingo Méndez-Álvarez², Alma D Paz-González²

¹Departamento de Parasitología, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Ciudad de México 11340, Mexico.

Molecules (Basel, Switzerland)

|April 14, 2026

Summary

This study repurposed FDA-approved drugs to find new treatments for Trypanosoma cruzi (T. cruzi) infections. Tadalafil, Zafirlukast, Raltegravir, and Olmesartan showed promising trypanocidal activity in vitro and in vivo.

Keywords:

Chagas disease FDA drugs molecular docking repositioning trypanothione synthetase

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In Vitro Drug Screening Against All Life Cycle Stages of Trypanosoma cruzi Using Parasites Expressing β-galactosidase

In Vitro Drug Screening Against All Life Cycle Stages of Trypanosoma cruzi Using Parasites Expressing β-galactosidase

Published on: November 5, 2021

Area of Science:

Parasitology and Drug Discovery
Computational Chemistry and Molecular Modeling

Background:

Chagas disease, caused by Trypanosoma cruzi (T. cruzi), lacks effective and safe treatments.
Drug repurposing offers a faster route to identify novel therapeutic agents.

Purpose of the Study:

To identify new anti-T. cruzi agents through drug repurposing.
To evaluate the efficacy of FDA-approved drugs against T. cruzi.

Main Methods:

Screening of 924 FDA-approved drugs using molecular docking against Trypanosoma cruzi trypanothione synthetase (TcTS).
In vitro and in vivo assays to evaluate the trypanocidal activity of selected compounds.
Molecular dynamics simulations (MDS) to elucidate the mechanism of action.

Main Results:

Tadalafil, Zafirlukast, Raltegravir, and Olmesartan demonstrated superior in vitro trypanocidal activity compared to Benznidazole and Nifurtimox.
These drugs reduced parasitemia by 20-50% in a murine model.
MDS suggested a mechanism involving the inhibition of TcTS.

Conclusions:

Repurposing Tadalafil, Zafirlukast, Raltegravir, and Olmesartan shows potential for developing new anti-T. cruzi therapies.
Targeting TcTS is a viable strategy for anti-T. cruzi drug development.