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PreprintCopyright
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Embargo date
2040-12-31
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- MG - IRR - Preprint [62]
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EXPLORATORY STUDY OF GUANIDINE DERIVATIVES AS NOVEL ANTI TRYPANOSOMA CRUZI SCAFFOLDS
Trypanosoma cruzi
Guanidines
In vitro trypanocidal activity
Cytotoxic assays
Author
Affilliation
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 diseaseTrypanosoma cruzi
Guanidines
In vitro trypanocidal activity
Cytotoxic assays
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