Journal article

Isoxazoles: synthesis, evaluation and bioinformatic design as acetylcholinesterase inhibitors

Margarita Gutierrez, Maria Francisca Matus, Tomas Poblete, Jessica Amigo, Gabriel Vallejos, Luis Astudillo

Journal of Pharmacy and Pharmacology | WILEY | Published : 2013

Abstract

OBJECTIVES: Inhibition of acetylcholinesterase (AChE) is a common treatment for early stages of Alzheimer's disease. In this study, nine isoxazoles derivatives were tested for their in-vitro AChE activity. The molecular docking showed the interaction of the compounds with the active site. METHODS: The isoxazoles were synthesized using 1,3-dipolar cycloaddition in the presence of sodium hypochlorite. They were also isolated and characterized by spectroscopic methods. The in-vitro activity was measured by an adapted version of Ellman's assay. KEY FINDINGS: The isoxazoles are described as inhibitors of AChE. The most potent compound in the series exhibited a moderate inhibitory activity (50% in..

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Grants

Awarded by Fondecyt


Awarded by Universidad de Talca


Funding Acknowledgements

We are grateful to the Fondecyt 1 100 481 project for financial support. The authors thank the grant from Universidad de Talca-VAC600-569.