New imidazole-based compounds active against Trypanosoma cruzi.

This study screened several imidazole-based compounds for anti-Trypanosoma potential. Using 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. All test compounds demonstrated interesting trypanocidal potential with IC50 values in the µM range (1amplt; 1C50 amplt;8 µM). The activities of the test compounds compared favorably with BZN, which had an IC50 value ca. 30 µM. Conversely, most of the test compounds were highly cytotoxic, resulting in selectivity lower than that of BZN (SI ampgt; 9.42). 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. PMID: 28071587 [PubMed - as supplied by publisher]
Source: Combinatorial Chemistry and High Throughput Screening - Category: Chemistry Authors: Tags: Comb Chem High Throughput Screen Source Type: research