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Letters in Drug Design & Discovery

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ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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Research Article

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

Author(s): Serry Atta El Bialy, Basem Mansour*, Waleed Abdelhakeem Bayoumi, Amira Taman and Hassan Mohammed Eissa

Volume 17, Issue 11, 2020

Page: [1432 - 1438] Pages: 7

DOI: 10.2174/1570180817999200523181211

Price: $65

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

Results and Discussions: 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.

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