Novel 2-(5-Aryl)thiophen-2-yl)benzimidazoles; Design, Synthesis and In vitro Evaluation Against Cercarial Phase of Schistosoma mansoni

(E-pub Ahead of Print)

Author(s): Serry A. El Bialy, Basem Mansour*, Waleed A. Bayoumi, Amira Taman, Hassan M. Eissaa

Journal Name: Letters in Drug Design & Discovery

Become EABM
Become Reviewer


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 cercaria.

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.

Keywords: Shistosoma, Benzimidazoles, Cercarial Assay, thiophene, Suzuki-Miyaura, Anthelmintic.

Rights & PermissionsPrintExport Cite as

Article Details

(E-pub Ahead of Print)
DOI: 10.2174/1570180817999200523181211
Price: $95

Article Metrics

PDF: 1