Synthesis and Evaluation of the Schistosomicidal and Trypanocidal Properties of Thioxo-Imidazolidines and Thiazolidin-2, 4-Diones

Aims: Synthesis and evaluation of the schistosomicidal and trypanocidal properties of thioxo-imidazolidines and thiazolidin-2,4-diones.

Study Design: We tested this compounds by way of in vitro evaluation against the adult worms of Schistosoma mansoni and forms of Trypanosoma cruzi.

Place and Duration of Study: Departamento de Antibióticos, Universidade Federal de Pernambuco and Fundação Oswaldo Cruz/PE between January 2013 and March 2014.

Methodology: This study was approved by the Ethics Committee on Animal Use Research authorized by the license number. 38/2012. The thiazolidine (5a-h) and imidazolidine (7a-d) compounds tested for its cytotoxicity to mouse splenocytes. Then the compounds were evaluated against adult worms of S. mansoni by performing the activity in vitro at doses 5-100 µg/mL. In addition, the derivatives were evaluated against epimastigote and trypomastigote forms of Trypanosoma cruzi (1.23-100 µg/mL).

Results: It was found that 7a derivate imidazolidine and 5f thiazolidine caused a high efficiency in terms of the mortality of S. mansoni (100%) in the first 24 hours of the experiment. In the trypanocidal activity, the thiazolidine compounds 5f and 5h exhibited satisfactory activity through their high effectiveness against the epimastigote (0.98 and 1.36 μg/mL) and trypomastigote (0.43 and 1.58 μg/mL) forms. Of the imidazolidine compound tested, derivative 7d stood out from the others in terms of its activity against the trypomastigote form, with IC50 of 1.26 μg/mL.

Conclusion: The imidazolidine and thiazolidine derivatives tested are potential schistosomicidal and trypanocidal drugs, although more advanced experiments involving in vivo assays are still required.