Abstract
Four diamines and three amino alcohols derived from 1-decanol, 1-dodecanol and 1,2-dodecanediol were evaluated in an in vitro assay against a mixture of trypomastigote and intracellular amastigote forms of Trypanosoma cruzi. Two of these compounds (6 and 7) showed better activity against both proliferative stages of T. cruzi than the positive control benznidazole, three were of similar potency (1, 2 and 5) and two were less active (3 and 4).
Highlights
Chagas disease is a neglected disease caused by the intracellular parasite Trypanosoma cruzi and affects mostly poor, rural and neglected populations, representing one of the main public health problems in the developing countries of Latin America (Clayton 2010)
We have shown in previous studies that lipophilic diamine and amino alcohol derivatives display inhibitory effects against Leishmania, Trichomonas vaginalis (Giordani et al 2009), Mycobacterium tuberculosis and on bloodstream trypomastigote forms of T. cruzi (Júnior et al 2010)
We described the trypanocidal activity of lipophilic diamines and amino alcohols on bloodstream trypomastigotes, with all the tested compounds displaying an activity ranging from IC50 values of 147 to 1,020 μΜ (Júnior et al 2010)
Summary
Chagas disease is a neglected disease caused by the intracellular parasite Trypanosoma cruzi and affects mostly poor, rural and neglected populations, representing one of the main public health problems in the developing countries of Latin America (Clayton 2010). The current treatment for Chagas disease consists of nifurtimox and benznidazole, which were developed more than four decades ago (Coura & de Castro 2002). These nitro compounds are considered far from ideal due to their multiple side effects and limited efficacy, in patients suffering from the chronic form of Chagas disease (Rocha et al 2007, Soeiro et al 2009). These limitations highlight the urgent need for new trypanocidal compounds to replace the existing chemotherapy drugs
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