Background: Current drugs available for the treatment of Chagas disease are fraught with
several challenges including severe toxicity and limited efficacy. These factors coupled with the
absence of effective drugs for treating the chronic stage of the disease have rendered the development
of new drugs against Chagas disease a priority.
Objective: This study screened several imidazole-based compounds for anti-Trypanosoma potential.
Method: Using an in vitro experimental infection model, several imidazole-based compounds were
screened for anti-proliferative effect on Trypanosoma cruzi epimastigotes. Additionally, all test
compounds were evaluated for unspecific cytotoxicity on L929 murine fibroblasts. Benznidazole
(BZN) served as reference drug.
Results: All test compounds demonstrated interesting trypanocidal potential with IC50
values in the μM
range (1< 1C50
<8 μM). The activities of the test compounds compared favorably with BZN, which had
value ca. 30 μM. Conversely, most of the test compounds were highly cytotoxic, resulting in
selectivity lower than that of BZN (SI > 9.42).
Conclusion: We provide evidence which implicate the imidazole-based compounds as potential
prototypes for the development of anti-parasitic agents. Findings have far-reaching relevance to drug
discovery efforts for trypanosomiasis.