Trypanocidal activity of chromenepyrazole derivatives

Andrade, Josimara Souza; Sales, Policarpo Ademar; Pereira, Fabio Junio; Murta, Silvane Maria Fonseca; Corrêa, Rodrigo S.; Taylor, Jason G.

doi:10.1007/s11696-022-02283-0

Cited by 2 publications

(3 citation statements)

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“…Thus, with the target compounds in hand, in vitro bioassays using trypomastigote and amastigote forms of Y-strain T. cruzi of β-galactosidase transfected the Tulahuen strain of T. cruzi. The whole cell-based approach is an ideal screening methodology given that it enables the evaluation of bioactive compounds against anti T. cruzi activity in infected cells whilst simultaneously monitoring their effects on both amastigotes and trypomastigotes in the same system [20][21][22][23]. Benznidazole was used as a positive control against T. cruzi (IC 50 = 3.81 µM, CC 50 = 2381 µM, and SI = 625) and cytotoxicity was determined in mammalian L929 cells (Table 1).…”

Section: Resultsmentioning

confidence: 99%

“…TLC analyses were performed using silica gel plates using ultraviolet light (254 nm), phosphomolybdic acid, or vanillin solution for visualization. The melting points were uncorrected and were recorded on a Buchi B-540 apparatus [23]. 1 H and 13 C NMR spectra were acquired using a Bruker DRX 400 MHz instrument ( 1 H at 400 MHz, 13 C at 100 MHz).…”

Section: Methodsmentioning

confidence: 99%

“…The in vitro anti-T. cruzi activity was evaluated on L929 cells (mouse fibroblasts) infected with the Tulahuen strain of the parasite expressing the Escherichia coli β-galactosidase as a reporter gene [23]. Briefly, for the bioassay, 4000 L929 cells were added to each well of a 96-well microtiter plate.…”

Section: Anti-trypanosoma Cruzi Activity Assay (Amastigotes and Trypo...mentioning

confidence: 99%

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In Vitro Evaluation of Arylsulfonamide Derivatives against Trypanosoma cruzi

Sales

Murta

Taylor

2023

DDC

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Chagas disease is caused by the parasite protozoan Trypanosoma cruzi (T. cruzi) and affects millions of people in over 21 countries in around the world. The main forms of treatment of this disease, benznidazole and nifurtimox, present low cure rates in the chronic phase and often have serious side effects. Herein, we describe the evaluation of the trypanocidal activity of arylsulfonamides. The arylsulfonamides were evaluated in vitro against the amastigote and trypomastigote forms of the parasite. An enantiomerically pure example of arylsulfonamide was also tested. The initial results suggest that the arylsulfonamides evaluated act as DNA binding agents. A moderate activity was monitored against the intracellular forms of T. cruzi, with the best compound exhibiting an IC50 value at 22 μM and a selectivity index of 120. However, the level of activity was not favorable for progressing towards in vivo studies for Chagas disease.

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Section: Resultsmentioning

confidence: 99%