In vitro antischistosomal activity of 2-aroyl-benzofuran derivatives against Schistosoma mansoni

Five 2-aroylbenzofurans were synthesized by condensation between α-bromoacetone and an ortho-hydroxybenzaldehyde or ortho-hydroxy-acetophenone and evaluated for their in vitro antischistomal effects against adult Schistosoma mansoni worms. Below 200 µg/mL, none of the tested 2-aroylbenzofurans killed adult S. mansoni worms. On the other hand, at 200 µg/mL all the tested compounds reduced the motor activity of adult S. mansoni worms after treatment for 72 h. At 200 µg/mL, compound 1 was the only one to decrease the motor activity of 67% of the worms after incubation for 24 h. The methyl group at C6 and the nature of the substituent at ring A play important roles in the efficacy of 2-aroylbenzofurans in reducing the worm motor activity.