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  • Therapeutic potential of selanyl amide derivatives in the in vitro anticholinesterase activity and in in vivo antiamnesic action.

Therapeutic potential of selanyl amide derivatives in the in vitro anticholinesterase activity and in in vivo antiamnesic action.

Canadian journal of physiology and pharmacology (2019-12-11)
Ethel A Wilhelm, Marina Laura C P Torres, Caroline F Pereira, Ane G Vogt, Rodrigo Cervo, Brenda G T Dos Santos, Roberta Cargnelutti, Cristiane Luchese
摘要

The present study evaluated the in vitro acetylcholinesterase (AChE) inhibitor activity of two new selanyl amide derivatives in cerebral structures of mice. Our results demonstrated that N-(2-(3-(phenylselanyl)propoxy)phenyl)furan-2-carboxamide (1) and N-(2-(3-(phenylselanyl)propoxy)phenyl)thiophene-2-carboxamide (2) inhibited the in vitro AChE activity in mice. Another objective was to assess the effect of the best AChE inhibitor in an amnesic model induced by scopolamine (SCO) in male Swiss mice. The involvement of AChE activity and lipid peroxidation in the cerebral structures was investigated. Our results showed that compound 1 (10 mg/kg, intragastrically) attenuated the latency to find the escape box and the number of holes visited in the Barnes maze task, without altering the locomotor and exploratory activities in an open-field test. Compound 1 protected against increasing in lipid peroxidation levels and AChE activity caused by SCO in the cerebral cortex and hippocampus of mice. In conclusion, the present study evidenced the in vitro anticholinesterase effect of two new selanyl amide derivatives in the cerebral structures of mice. Moreover, compound 1, a selanyl amide derivative containing a furan ring, demonstrated antiamnesic action due to its antioxidant and anticholinesterase activities in cerebral structures.

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Sigma-Aldrich
呋喃甲酰氯, 95%