Journal
BIOORGANIC CHEMISTRY
Volume 81, Issue -, Pages 134-143Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2018.08.009
Keywords
2-amino-4H-pyrans; Alzheimer's disease; AChE; BChE; Molecular docking simulations
Funding
- Deanship of Scientific Research at King Saud University [RG-1438-052]
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Novel highly functionalized 2-amino-4H-pyrans were achieved in excellent yields under simple grinding at ambient temperature and were assessed for their potential for treating Alzheimer's disease (AD). The 2-amino-4H-pyran bearing nitro groups on both the aryl rings showed the highest activity, with an IC50 of 1.98 +/- 0.09 mu M against acetylcholinesterase (AChE) and 10.62 +/- 0.21 mu M against butyrylcholinesterase (BChE), the inhibition mechanisms on AChE and BChE receptors were revealed by means of molecular docking simulations.
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