Exploratory Study of Guanidine Derivatives as Novel Anti Trypanosoma cruzi Scaffolds

How to cite: Zampieri, E. H.; Junior, P. A. S.; Murta, S. M. F.; Kalaba, P.; Prado-Roller, A.; Gajic, N.; Zehl, M.; Fabisikova, A.; dos Anjos, L. R.; Gushiken, L. P.; Lubec, G.; Gonzalez, E. R. P. Exploratory Study of Guanidine Derivatives as Novel Anti Trypanosoma cruzi Scaffolds. Preprints 2024, 2024071775. https://doi.org/10.20944/preprints202407.1775.v1 Zampieri, E. H.; Junior, P. A. S.; Murta, S. M. F.; Kalaba, P.; Prado-Roller, A.; Gajic, N.; Zehl, M.; Fabisikova, A.; dos Anjos, L. R.; Gushiken, L. P.; Lubec, G.; Gonzalez, E. R. P. Exploratory Study of Guanidine Derivatives as Novel Anti Trypanosoma cruzi Scaffolds. Preprints 2024, 2024071775. https://doi.org/10.20944/preprints202407.1775.v1

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MDPI and ACS Style

Zampieri, E. H.; Junior, P. A. S.; Murta, S. M. F.; Kalaba, P.; Prado-Roller, A.; Gajic, N.; Zehl, M.; Fabisikova, A.; dos Anjos, L. R.; Gushiken, L. P.; Lubec, G.; Gonzalez, E. R. P. Exploratory Study of Guanidine Derivatives as Novel Anti Trypanosoma cruzi Scaffolds. Preprints 2024, 2024071775. https://doi.org/10.20944/preprints202407.1775.v1

APA Style

Zampieri, E. H., Junior, P. A. S., Murta, S. M. F., Kalaba, P., Prado-Roller, A., Gajic, N., Zehl, M., Fabisikova, A., dos Anjos, L. R., Gushiken, L. P., Lubec, G., & Gonzalez, E. R. P. (2024). Exploratory Study of Guanidine Derivatives as Novel Anti <i>Trypanosoma cruzi</i> Scaffolds. Preprints. https://doi.org/10.20944/preprints202407.1775.v1

Chicago/Turabian Style

Zampieri, E. H., Gert Lubec and Eduardo Rene Perez Gonzalez. 2024 "Exploratory Study of Guanidine Derivatives as Novel Anti <i>Trypanosoma cruzi</i> Scaffolds" Preprints. https://doi.org/10.20944/preprints202407.1775.v1

Abstract

Chagas disease (CD) is a neglected tropical parasitic disease caused by the protozoan Trypanosoma cruzi. Unfortunately, the current etiological treatment for CD is unsatisfactory, due to the high toxicity and low cure efficacy of compounds, mainly during the chronic phase of this disease. Thus, the discovery of new drugs for the treatment of CD is urgent. In the present study, we report the synthesis of a series of guanidines and its evaluation in in vitro assays to determine the trypanocidal effects on the Tulahuen T. cruzi strain, transfected with a β-galactosidase reporter gene, in comparison to the cytotoxic effects on vertebrate cells. The most potent and selective compounds LQOF-G1 and LQOF-G29 were considered good drug prototypes and candidates for in vivo tests using mice. Both compounds possess an electron withdrawing group on the aniline moiety, namely a NO2 and Br group, respectively, which effectively decrease the electron density. LQOF-G29 stands out among the investigated compounds due to the replacement of the benzyl group by methyladamantane.

Keywords

Chagas disease; Trypanosoma cruzi; guanidines; in vitro trypanocidal activity; cytotoxic assays

Subject

Chemistry and Materials Science, Medicinal Chemistry

Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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