1. Highly functionalized 2-amino-4H-pyrans as potent cholinesterase inhibitors.
- Author
-
Kumar, Raju Suresh, Almansour, Abdulrahman I., Arumugam, Natarajan, Al-thamili, Dhaifallah M., Basiri, Alireza, Kotresha, D., Manohar, Thota Sai, Venketesh, S., Asad, Mohammad, and Asiri, Abdullah M.
- Subjects
- *
PYRAN , *CHOLINESTERASE inhibitors , *ALZHEIMER'S disease treatment , *GROUP 15 elements , *NUCLEAR magnetic resonance spectroscopy , *MOLECULAR docking - Abstract
Graphical abstract Highly functionalized 2-amino-4 H -pyrans were achieved in excellent yields and assessed for their potential as inhibitors of AD. Compound bearing nitro groups on both the aryl rings showed the highest activity and this is also supported by its inhibition mechanisms on AChE and BChE receptors. Highlights • Novel highly functionalized 2-amino-4 H -pyrans were achieved in excellent yields. • The structure of 4 H -pyrans were confirmed by FT-IR and NMR spectroscopic studies. • The compounds were evaluated as potential agents for Alzheimer's disease. • Molecular docking simulation was performed to disclose the mechanism of inhibition. Abstract Novel highly functionalized 2-amino-4 H -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-4 H -pyran bearing nitro groups on both the aryl rings showed the highest activity, with an IC 50 of 1.98 ± 0.09 µM against acetylcholinesterase (AChE) and 10.62 ± 0.21 µM against butyrylcholinesterase (BChE), the inhibition mechanisms on AChE and BChE receptors were revealed by means of molecular docking simulations. [ABSTRACT FROM AUTHOR]
- Published
- 2018
- Full Text
- View/download PDF