Purine derivatives as potential agents against Chagas disease: Ex vivo, in vitro, in silico evaluation, and identification of targets in Trypanosoma cruzi

= 13.5 and 19.6 µM, respectively), which was more closely aligned with trypanocidal activity. In addition, 9i and 9t did not bind to TcBDF3, indicating selectivity among these targets. Molecular docking and 200 ns molecular dynamics simulations supported the stable binding of purine 9i to the TcBDF2 bromodomain pocket. In addition, purines 9i, 9j, 9m, and 9t were predicted to have good pharmacokinetic profiles for oral administration of the drug. Overall, trisubstituted purines emerged as promising antichagasic leads, with TcBDF2 engagement appearing more consistent with the observed trypanocidal activity, thereby guiding future optimisation towards a balance of potency, selectivity, and cytotoxicity.

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Publication Details

Journal
Biomedicine & Pharmacotherapy
Published
2026-06-09
DOI
https://doi.org/10.1016/j.biopha.2026.119636
Primary Topic
Trypanosoma species research and implications
Type
article
Field-Weighted Citation Impact
0.00

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article

Purine derivatives as potential agents against Chagas disease: Ex vivo, in vitro, in silico evaluation, and identification of targets in Trypanosoma cruzi

Thalía Delgado, Emir Salas‐Sarduy, Cristian O. Salas, Mercedes Didier Garnham et al.
Biomedicine & Pharmacotherapy
Trypanosoma species research and implications
article

Purine derivatives as potential agents against Chagas disease: Ex vivo, in vitro, in silico evaluation, and identification of targets in Trypanosoma cruzi

Thalía Delgado, Emir Salas‐Sarduy, Cristian O. Salas, Mercedes Didier Garnham, Rogelio Gómez-Escobedo, Jean-Luc Bertrand, Alonzo González-González, Benjamín Nogueda-Torres, Gildardo Rivera, Esteban Serra, Victoria Alonso
article en

Abstract

= 13.5 and 19.6 µM, respectively), which was more closely aligned with trypanocidal activity. In addition, 9i and 9t did not bind to TcBDF3, indicating selectivity among these targets. Molecular docking and 200 ns molecular dynamics simulations supported the stable binding of purine 9i to the TcBDF2 bromodomain pocket. In addition, purines 9i, 9j, 9m, and 9t were predicted to have good pharmacokinetic profiles for oral administration of the drug. Overall, trisubstituted purines emerged as promising antichagasic leads, with TcBDF2 engagement appearing more consistent with the observed trypanocidal activity, thereby guiding future optimisation towards a balance of potency, selectivity, and cytotoxicity.

Biomedicine & PharmacotherapyVol. 200
Pontificia Universidad Católica de Chile (CL), National University of General San Martín (AR), Instituto de Biología Molecular y Celular de Rosario (AR), Instituto Politécnico Nacional (MX)
Fondo Nacional de Desarrollo Científico y Tecnológico
Openalex Percentile: Top 7%
Trypanosoma species research and implications
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