Background: literature survey has pointed out that Benzimidazoles represent an interesting class of
anthelmintics of which several potent members were developed.
Objective: Benzimidazoles hybridized with
pharmacophoric moieties possessing anthelmintic activity were designed, synthesized to be evaluated against
Methods: Structural modification was achieved through 2- and 5-positions. Moreover, in vitro
cercarial assay was adopted to evaluate target compounds.
Results: Biological screening revealed that
compound 3h showed significant activity with survival index of 35% at a 100 µg/mL concentration. Whereas,
compounds 3a and 3c showed moderate activity, the rest of tested compounds exhibited low activity.
Conclusion: The current study evidenced that the new hybrids "benzimidazole-thiophen-aryl" are successful as
cercacidal agents. Further studies of this novel tri-ring systems are suggested on adult worms of S. Mansoni.