Journal
BIOORGANIC CHEMISTRY
Volume 83, Issue -, Pages 303-316Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2018.10.056
Keywords
Alzheimer's disease; Tacrine-Coumarins; 1,2,3-Triazole; Docking study; Dual binding site; Morris water maze
Funding
- Research Council of Tehran University of Medical Sciences [94-01-33-28713]
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A new series of tacrine-coumarin hybrids linked to 1,2,3-triazole were designed, synthesized, and tested as potent dual binding site cholinesterase inhibitors (ChEIs) for the treatment of Alzheimer's disease (AD). Among them, compound 8e was the most potent anti-AChE derivative (IC50 = 27 nM) and compound 8m displayed the best anti-BChE activity (IC50 = 6 nM) much more active than tacrine and donepezil as the reference drugs. Compound 8e was also evaluated for its BACE1 inhibitory activity and neuroprotectivity against PC12 cells exposed to A beta(25-35) which indicated low activity. Finally, in vivo studies by Morris water maze task showed that compound 8e significantly reversed scopolamine-induced memory deficit in rats.
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