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08 July 2017 : Laboratory Research  

Design and Development of a Novel Chalcone Derivative as an Anticholinesterase Inhibitor for Possible Treatment of Dementia

Fu-Chun Zhao1B, Yan Wu2DE, Xiao-Jie Song1A*

DOI: 10.12659/MSM.901842

Med Sci Monit 2017; 23:3311-3317

Abstract

BACKGROUND: Cognitive decline (e.g., memory loss), which mainly occurs in the elderly, is termed dementia. In the present study, we intended to explore the cholinesterase inhibitory activity of some novel synthesized chalcones, together with their effect on β-amyloid anti-aggregation.

MATERIAL AND METHODS: A novel class of chalcone derivatives have been synthesized and characterized by FT-IR, ¹H-NMR, ¹³C-NMR, and mass and elemental analysis. These derivatives were later used for the determination of acetylcholinesterase (AChE) inhibitory and b-amyloid anti-aggregation activity.

RESULTS: The results of the study showed that among the developed compounds, 8g inhibits AChE more prominently than BuChE, as suggested by a selectivity index (SI) of 2.88. Furthermore, the most potent compound, 8g, showed considerable action in inhibition of β-secretase and Aβ aggregation, but not as prominent as that of curcumin as a standard.

CONCLUSIONS: In conclusion, our study revealed a novel class of chalcone derivatives as a selective inhibitor of AChE with considerably action against β-secretase and Aβ aggregation. Our results may be useful in developing AD drug therapy and warrant further investigation to generate more advanced analogues.

Keywords: Alzheimer Disease, Cholinesterase Inhibitors, Chemistry Techniques, Synthetic

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Editorial

01 December 2023 : Editorial  

Editorial: Outbreaks of Post-Pandemic Childhood Pneumonia and the Re-Emergence of Endemic Respiratory Infections

Dinah V. Parums
Science Editor, Medical Science Monitor, International Scientific Information, Inc., Melville, NY, USA

DOI: 10.12659/MSM.943312

Med Sci Monit 2023; 29:e943312

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Medical Science Monitor eISSN: 1643-3750
Medical Science Monitor eISSN: 1643-3750