Anthelmintic Effects of Alkylated Diamines and Amino Alcohols againstSchistosoma mansoni

Abstract

Polyamines are substances involved in many aspects of cell growth, division, and differentiation. Because of the metabolic differences between host cells and parasite cells, polyamine metabolism has been considered as a potential target for the chemotherapy of parasitic diseases. The aim of this work was to evaluate the schistosomicidal activity of differentN-alkylated diamines (3a–3h), amino alcohols (4a–4d), and glycosylated amino alcohols (10a–10d). Compounds were prepared by synthetic methods and submitted toin vitroevaluation against adult worms ofSchistosoma mansoni. At 100 μM,3b,3e, and3has well as4a,4b,4d,10a,10b, and10dresulted in 100% mortality of adult schistosomes. Compound3d(12.5 to 100 μM) caused the death of 100% of both male and female adult schistosomes, while3f(12.5 to 100 μM) resulted in 100% mortality of only male adult worms, whereas no mortality in female worms was observed. Compounds3dand3fwere also able to reduce viability and decrease production of developed eggs in comparison with the negative control group. Diamines3dand3fmay represent useful lead compounds for further optimization in order to develop new schistosomicidal agents.