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

[ Vol. 17 , Issue. 11 ]

Author(s):

Serry A. El Bialy, Basem Mansour*, Waleed A. Bayoumi, Amira Taman and Hassan M. Eissa   Pages 1432 - 1438 ( 7 )

Abstract:


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 and Discussions: Structural modification was achieved through 2- and 5-positions. Moreover, an in vitro cercarial assay was adopted to evaluate target compounds.

Results: Biological screening revealed that compound 3h showed significant activity with a survival index of 35% at a 100 μg/mL concentration. Whereas, compounds 3a and 3c showed moderate activity, the rest of the 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 system are suggested on adult worms of S. mansoni.

Keywords:

Anthelmintic, benzimidazoles, cercarial assay, Schistosoma, suzuki-miyaura, thiophene.

Affiliation:

Pharmaceutical Organic Chemistry Dept., Faculty of Pharmacy, Mansoura University, Mansoura 35516, Pharmaceutical Organic Chemistry Dept., Faculty of Pharmacy, Mansoura University, Mansoura 35516, Pharmaceutical Organic Chemistry Dept., Faculty of Pharmacy, Mansoura University, Mansoura 35516, Medical Parasitology Dept., Faculty of Medicine, Mansoura University, Mansoura 35516, Pharmaceutical Organic Chemistry Dept., Faculty of Pharmacy, Mansoura University, Mansoura 35516



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