Synthesis and Docking Studies of a Novel Tetrahydroquinazoline Derivative as Promising Scaffold for Acetylcholine Esterase Inhibition | ||
| Egyptian Journal of Chemistry | ||
| Article 13, Volume 63, Issue 12, December 2020, Pages 4797-4804 PDF (1.37 M) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/ejchem.2020.27985.2588 | ||
| Authors | ||
| Rawan A. Alsuhaimat1; Qais Abualassal2; zead abudyah3; Sherif S. Ebada4; Amgad Albohy* 5 | ||
| 1Faculty of Pharmacy, Mu’tah University, Al-Karak, 61166, Amman, Jordan | ||
| 2Department of Applied Pharmaceutical Sciences, Faculty of Pharmacy, Isra University, Amman, Jordan | ||
| 3Faculty of pharmacy / AL-isra university Amman / Jordan | ||
| 4Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mu’tah University, Al-Karak, Jordan. and Department of Pharmacognosy, Faculty of Pharmacy, Ain-Shams University, Cairo, Egypt | ||
| 5Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The British University in Egypt (BUE), Egypt | ||
| Abstract | ||
| Alzheimer’s disease (AD) is one of the most prevalent neurodegenerative disorder. While pathological hallmarks of this disorder are known, the exact cause of AD remains unclear. Quinazoline was found to be a promising scaffold for the design and development of Acetylcholinesterase (AChE) inhibitors. In this study we report the synthesis of 1'-methyl-3', 4'-dihydro1'H-spiro[cyclopentane-1, 2'-quinazoline] (4) in 73.3% yield. The structure of compound 4 was confirmed with GC-MS, 1H and 13C-NMR. Acetylcholine esterase inhibition was studied virtually with docking into AChE active site and suggests potential use of 4 as a promising scaffold for acetylcholine esterase inhibitor design which might be useful for Alzheimer’s disease. | ||
| Keywords | ||
| Acetylcholine esterase inhibitor; Alzheimer disease; Quinazoline derivatives; Spiro compounds; Molecular Docking | ||
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